IP6K2
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Summary
IP6K2 (inositol hexakisphosphate kinase 2, HGNC:17313) is a protein-coding gene on chromosome 3p21.31, encoding Inositol hexakisphosphate kinase 2 (Q9UHH9). Converts inositol hexakisphosphate (InsP6) to diphosphoinositol pentakisphosphate (InsP7/PP-InsP5).
This gene encodes a protein that belongs to the inositol phosphokinase (IPK) family. This protein is likely responsible for the conversion of inositol hexakisphosphate (InsP6) to diphosphoinositol pentakisphosphate (InsP7/PP-InsP5). It may also convert 1,3,4,5,6-pentakisphosphate (InsP5) to PP-InsP4 and affect the growth suppressive and apoptotic activities of interferon-beta in some ovarian cancers. Alternative splicing results in multiple transcript variants encoding different isoforms.
Source: NCBI Gene 51447 — RefSeq curated summary.
At a glance
- GWAS associations: 28
- Clinical variants (ClinVar): 55 total
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_016291
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:17313 |
| Approved symbol | IP6K2 |
| Name | inositol hexakisphosphate kinase 2 |
| Location | 3p21.31 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000068745 |
| Ensembl biotype | protein_coding |
| OMIM | 606992 |
| Entrez | 51447 |
Gene structure
Transcript identifiers
Ensembl transcripts: 59 — 52 protein_coding, 3 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined, 2 retained_intron
ENST00000328631, ENST00000340879, ENST00000412795, ENST00000412850, ENST00000413298, ENST00000413654, ENST00000416707, ENST00000417896, ENST00000424035, ENST00000431721, ENST00000432678, ENST00000433104, ENST00000434860, ENST00000436134, ENST00000437427, ENST00000440424, ENST00000443853, ENST00000443964, ENST00000446860, ENST00000449563, ENST00000449610, ENST00000450045, ENST00000453202, ENST00000454335, ENST00000455545, ENST00000476645, ENST00000479914, ENST00000491686, ENST00000904743, ENST00000904744, ENST00000904745, ENST00000904746, ENST00000904747, ENST00000904748, ENST00000904749, ENST00000904750, ENST00000904751, ENST00000921847, ENST00000921848, ENST00000921849, ENST00000921850, ENST00000921851, ENST00000921852, ENST00000921853, ENST00000921854, ENST00000921855, ENST00000921856, ENST00000921857, ENST00000946876, ENST00000946877, ENST00000946878, ENST00000946879, ENST00000946880, ENST00000946881, ENST00000946882, ENST00000946883, ENST00000946884, ENST00000946885, ENST00000946886
RefSeq mRNA: 8 — MANE Select: NM_016291
NM_001005909, NM_001005910, NM_001005911, NM_001146178, NM_001146179, NM_001190316, NM_001190317, NM_016291
CCDS: CCDS2777, CCDS33752, CCDS54579, CCDS54580, CCDS54581
Canonical transcript exons
ENST00000328631 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001819400 | 48688003 | 48688773 |
| ENSE00001929186 | 48717157 | 48717221 |
| ENSE00003486624 | 48689538 | 48689713 |
| ENSE00003585030 | 48691307 | 48691482 |
| ENSE00003589067 | 48695090 | 48695421 |
| ENSE00003604107 | 48692954 | 48693179 |
Expression profiles
Bgee: expression breadth ubiquitous, 275 present calls, max score 98.71.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 40.0029 / max 380.6294, expressed in 1815 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 42172 | 39.7896 | 1815 |
| 42169 | 0.2133 | 95 |
Top tissues by expression
283 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right hemisphere of cerebellum | UBERON:0014890 | 98.71 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 98.69 | gold quality |
| cerebellar cortex | UBERON:0002129 | 98.64 | gold quality |
| ganglionic eminence | UBERON:0004023 | 98.52 | gold quality |
| tibial nerve | UBERON:0001323 | 98.44 | gold quality |
| skin of abdomen | UBERON:0001416 | 98.29 | gold quality |
| skin of leg | UBERON:0001511 | 98.28 | gold quality |
| right uterine tube | UBERON:0001302 | 98.23 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 98.20 | gold quality |
| body of uterus | UBERON:0009853 | 98.10 | gold quality |
| adenohypophysis | UBERON:0002196 | 97.94 | gold quality |
| metanephros cortex | UBERON:0010533 | 97.94 | gold quality |
| cortical plate | UBERON:0005343 | 97.92 | gold quality |
| cerebellum | UBERON:0002037 | 97.89 | gold quality |
| left ovary | UBERON:0002119 | 97.81 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 97.81 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 97.78 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 97.76 | gold quality |
| rectum | UBERON:0001052 | 97.75 | gold quality |
| transverse colon | UBERON:0001157 | 97.70 | gold quality |
| right adrenal gland | UBERON:0001233 | 97.67 | gold quality |
| endocervix | UBERON:0000458 | 97.66 | gold quality |
| right ovary | UBERON:0002118 | 97.55 | gold quality |
| minor salivary gland | UBERON:0001830 | 97.49 | gold quality |
| pituitary gland | UBERON:0000007 | 97.45 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 97.45 | gold quality |
| body of pancreas | UBERON:0001150 | 97.33 | gold quality |
| ectocervix | UBERON:0012249 | 97.29 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 97.20 | gold quality |
| thyroid gland | UBERON:0002046 | 97.14 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): SP1
miRNA regulators (miRDB)
32 targeting IP6K2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4283 | 100.00 | 66.42 | 2097 |
| HSA-MIR-3185 | 99.99 | 68.12 | 1959 |
| HSA-MIR-1-3P | 99.93 | 72.35 | 1914 |
| HSA-MIR-206 | 99.93 | 72.50 | 1893 |
| HSA-MIR-613 | 99.91 | 71.50 | 1710 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-202-3P | 99.84 | 71.41 | 1290 |
| HSA-MIR-24-3P | 99.59 | 69.97 | 1934 |
| HSA-MIR-105-5P | 99.54 | 69.24 | 2060 |
| HSA-MIR-7853-5P | 99.54 | 69.30 | 2055 |
| HSA-MIR-6833-5P | 99.50 | 68.93 | 1161 |
| HSA-MIR-409-3P | 99.50 | 66.33 | 1192 |
| HSA-MIR-4441 | 99.49 | 66.56 | 3216 |
| HSA-MIR-653-5P | 99.46 | 67.35 | 1300 |
| HSA-MIR-10522-5P | 99.26 | 68.50 | 2087 |
| HSA-MIR-661 | 99.09 | 65.94 | 2062 |
| HSA-MIR-4270 | 99.02 | 66.26 | 1987 |
| HSA-MIR-4709-3P | 98.88 | 68.04 | 1594 |
| HSA-MIR-583 | 98.71 | 67.44 | 1791 |
| HSA-MIR-9500 | 98.62 | 66.54 | 1845 |
| HSA-MIR-6754-5P | 98.60 | 65.54 | 1627 |
| HSA-MIR-211-3P | 98.14 | 66.77 | 1052 |
| HSA-MIR-4518 | 98.12 | 66.82 | 1030 |
| HSA-MIR-892B | 98.00 | 67.11 | 821 |
| HSA-MIR-1266-5P | 97.71 | 66.92 | 1052 |
| HSA-MIR-510-5P | 97.66 | 65.82 | 916 |
| HSA-MIR-3190-3P | 97.61 | 66.95 | 1406 |
| HSA-MIR-6736-3P | 96.98 | 65.22 | 1342 |
| HSA-MIR-12128 | 96.67 | 66.98 | 1471 |
| HSA-MIR-4491 | 96.53 | 66.20 | 935 |
Literature-anchored findings (GeneRIF, showing 12)
- IHPK2 over expression enhances sensitivity of ovarian carcinoma cells to radiation, IFN-beta, caspase 8 and DR4 (PMID:11896621)
- InsP6K2 is a physiologic mediator of cell death (PMID:15533939)
- IHPK2-TRAF2 binding leads to attenuation of TAK1- and NF-kappaB-mediated signaling and is partially responsible for the apoptotic activity of IHPK2. (PMID:17379600)
- Gene disruption of IP6K2 in colorectal cancer cells selectively impairs p53-mediated apoptosis, instead favoring cell-cycle arrest. IP6K2 acts by binding directly to p53 and decreasing expression of proarrest gene targets (PMID:21078964)
- Casein kinase-2 mediates cell survival through phosphorylation and degradation of inositol hexakisphosphate kinase-2. (PMID:21262846)
- Genetic polymorphisms in IP6K2 gene is associated with autoimmune disease. (PMID:22446964)
- FGF2-signaling involves the inositol polyphosphate cascade, including inositol hexakisphosphate kinase (IP6K), and demonstrate that IP6K1,2 regulates Runx2 and osteoblast gene expression. (PMID:23322705)
- An alpha-helical pair and a rare, two-turn 310 helix, that together form a substrate-binding pocket of IP6K2. (PMID:24956979)
- conclude that IP6K1 and -2 together control inositol pyrophosphate metabolism and thereby physiologically regulate phosphate export and other aspects of mammalian cellular phosphate homeostasis (PMID:31186349)
- LINC00467 knockdown repressed cell proliferation but stimulated cell apoptosis in glioblastoma via miR-339-3p/IP6K2 axis. (PMID:32176627)
- Inositol hexakisphosphate kinase 2 promotes cell death of anterior horn cells in the spinal cord of patients with amyotrophic lateral sclerosis. (PMID:32929655)
- Circ-IP6K2 suppresses tumor progression by modulating the miR-1292-5p/CAMK2N1 signal in clear cell renal cell carcinoma. (PMID:38980439)
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ip6k2a | ENSDARG00000008310 |
| danio_rerio | ip6k2b | ENSDARG00000019613 |
| mus_musculus | Ip6k2 | ENSMUSG00000032599 |
| rattus_norvegicus | Ip6k2 | ENSRNOG00000020361 |
| drosophila_melanogaster | IP3K1 | FBGN0032147 |
| drosophila_melanogaster | Ip6k | FBGN0034644 |
| caenorhabditis_elegans | lfe-2 | WBGENE00002979 |
| caenorhabditis_elegans | F30A10.3 | WBGENE00009262 |
Paralogs (6): ITPKC (ENSG00000086544), ITPKA (ENSG00000137825), ITPKB (ENSG00000143772), IPMK (ENSG00000151151), IP6K3 (ENSG00000161896), IP6K1 (ENSG00000176095)
Protein
Protein identifiers
Inositol hexakisphosphate kinase 2 — Q9UHH9 (reviewed: Q9UHH9)
Alternative names: P(i)-uptake stimulator
All UniProt accessions (15): Q9UHH9, B2RCP4, C9J124, C9J3W9, C9J536, C9J790, C9J8W6, C9JGK2, C9JHV2, C9JHX0, C9JLG7, C9JMC9, C9JRM0, C9JU99, F8WDQ5
UniProt curated annotations — full annotation on UniProt →
Function. Converts inositol hexakisphosphate (InsP6) to diphosphoinositol pentakisphosphate (InsP7/PP-InsP5).
Subcellular location. Nucleus.
Activity regulation. Inhibited by flavonoids, including myricetin, quercetin, luteolin, isorhamnetin, rhamnetin, kaempferol, diosmetin and apigenin.
Pathway. Phospholipid metabolism; phosphatidylinositol metabolism.
Miscellaneous. May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay.
Similarity. Belongs to the inositol phosphokinase (IPK) family.
Isoforms (6)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9UHH9-1 | 1 | yes |
| Q9UHH9-2 | 2 | |
| Q9UHH9-3 | 3 | |
| Q9UHH9-4 | 4 | |
| Q9UHH9-5 | 5 | |
| Q9UHH9-6 | 6 |
RefSeq proteins (8): NP_001005909, NP_001005910, NP_001005911, NP_001139650, NP_001139651, NP_001177245, NP_001177246, NP_057375* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR005522 | IPK | Family |
| IPR038286 | IPK_sf | Homologous_superfamily |
Pfam: PF03770
Enzyme classification (BRENDA):
- EC 2.7.4.21 — inositol-hexakisphosphate 5-kinase (BRENDA: 10 organisms, 35 substrates, 31 inhibitors, 11 Km, 1 kcat entries)
Substrate kinetics (BRENDA)
6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.037–1.4 | 4 |
| INOSITOL HEXAKISPHOSPHATE | 0.0007–0.0061 | 3 |
| 1D-MYO-INOSITOL HEXAKISPHOSPHATE | 0.0004 | 1 |
| 5-DIPHOSPHO-1D-MYO-INOSITOL (1,2,3,4,6)PENTAKISP | 0.002 | 1 |
| ADP | 1.57 | 1 |
| D-MYO-INOSITOL-1,3,4,5,6-PENTAKISPHOSPHATE | 0.0055 | 1 |
Catalyzed reactions (Rhea), 1 shown:
- 1D-myo-inositol hexakisphosphate + ATP = 5-diphospho-1D-myo-inositol 1,2,3,4,6-pentakisphosphate + ADP (RHEA:12793)
UniProt features (19 total): splice variant 10, binding site 6, sequence conflict 2, chain 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UHH9-F1 | 75.92 | 0.50 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (6): 207–209; 220; 222; 236–243; 383; 386
Function
Pathways and Gene Ontology
Reactome pathways
7 pathways
| ID | Pathway |
|---|---|
| R-HSA-1855191 | Synthesis of IPs in the nucleus |
| R-HSA-909733 | Interferon alpha/beta signaling |
| R-HSA-1280215 | Cytokine Signaling in Immune system |
| R-HSA-1430728 | Metabolism |
| R-HSA-1483249 | Inositol phosphate metabolism |
| R-HSA-168256 | Immune System |
| R-HSA-913531 | Interferon Signaling |
MSigDB gene sets: 244 (showing top):
AHRARNT_01, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_REGULATION_OF_PHOSPHORYLATION, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, RORA1_01, ATACCTC_MIR202, GOBP_NEGATIVE_REGULATION_OF_CELL_GROWTH, GOBP_INOSITOL_PHOSPHATE_METABOLIC_PROCESS, GOBP_PEPTIDYL_SERINE_MODIFICATION, GOBP_POLYOL_METABOLIC_PROCESS, GOBP_GROWTH, GOBP_REGULATION_OF_TRANSFERASE_ACTIVITY, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, AAAYRNCTG_UNKNOWN
GO Biological Process (11): negative regulation of cell growth (GO:0030308), inositol phosphate biosynthetic process (GO:0032958), positive regulation of apoptotic process (GO:0043065), inositol phosphate metabolic process (GO:0043647), phosphatidylinositol phosphate biosynthetic process (GO:0046854), protein stabilization (GO:0050821), positive regulation of protein K48-linked ubiquitination (GO:1902524), cellular response to flavonoid (GO:1905396), lipid metabolic process (GO:0006629), phosphatidylinositol metabolic process (GO:0046488), organophosphate biosynthetic process (GO:0090407)
GO Molecular Function (13): inositol-1,3,4,5,6-pentakisphosphate kinase activity (GO:0000827), inositol hexakisphosphate kinase activity (GO:0000828), diphosphoinositol pentakisphosphate kinase activity (GO:0000829), inositol hexakisphosphate 5-kinase activity (GO:0000832), ATP binding (GO:0005524), protein-containing complex binding (GO:0044877), inositol 5-diphosphate pentakisphosphate 5-kinase activity (GO:0052836), diphosphoinositol tetrakisphosphate kinase activity (GO:0052839), flavonoid binding (GO:0097243), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (5): fibrillar center (GO:0001650), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cell junction (GO:0030054)
Reactome top-level categories
Rollup of top-5 pathways:
| Category | Pathways |
|---|---|
| Inositol phosphate metabolism | 1 |
| Interferon Signaling | 1 |
| Immune System | 1 |
| Metabolism | 1 |
| Cytokine Signaling in Immune system | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| inositol phosphate kinase activity | 5 |
| cellular anatomical structure | 4 |
| phosphotransferase activity, phosphate group as acceptor | 3 |
| binding | 3 |
| organophosphate metabolic process | 2 |
| phosphotransferase activity, alcohol group as acceptor | 2 |
| regulation of cell growth | 1 |
| cell growth | 1 |
| negative regulation of growth | 1 |
| negative regulation of cellular process | 1 |
| inositol phosphate metabolic process | 1 |
| polyol biosynthetic process | 1 |
| organophosphate biosynthetic process | 1 |
| apoptotic process | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of programmed cell death | 1 |
| polyol metabolic process | 1 |
| glycerophospholipid biosynthetic process | 1 |
| regulation of protein stability | 1 |
| regulation of protein K48-linked ubiquitination | 1 |
| protein K48-linked ubiquitination | 1 |
| positive regulation of protein polyubiquitination | 1 |
| cellular response to oxygen-containing compound | 1 |
| response to flavonoid | 1 |
| primary metabolic process | 1 |
| phosphorus metabolic process | 1 |
| biosynthetic process | 1 |
| inositol hexakisphosphate kinase activity | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| nucleolus | 1 |
| intracellular membrane-bounded organelle | 1 |
| nuclear lumen | 1 |
| intracellular anatomical structure | 1 |
Protein interactions and networks
STRING
946 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| IP6K2 | PPIP5K1 | Q6PFW1 | 937 |
| IP6K2 | PPIP5K2 | O43314 | 879 |
| IP6K2 | POLR1F | Q3B726 | 773 |
| IP6K2 | DUSP16 | Q9BY84 | 701 |
| IP6K2 | FKBP4 | Q02790 | 695 |
| IP6K2 | ITPKB | P27987 | 670 |
| IP6K2 | ITPKA | P23677 | 651 |
| IP6K2 | IPPK | Q9H8X2 | 611 |
| IP6K2 | EXT2 | Q93063 | 600 |
| IP6K2 | HSP90AA1 | P07900 | 559 |
| IP6K2 | FKBP8 | Q14318 | 493 |
| IP6K2 | NKX2-1 | P43699 | 491 |
| IP6K2 | CCDC106 | Q9BWC9 | 476 |
| IP6K2 | LNX2 | Q8N448 | 474 |
| IP6K2 | CDC37 | Q16543 | 460 |
IntAct
29 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| IP6K2 | LNX2 | psi-mi:“MI:0915”(physical association) | 0.670 |
| LNX2 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.670 |
| IP6K2 | TP53 | psi-mi:“MI:0407”(direct interaction) | 0.600 |
| IP6K2 | TP53 | psi-mi:“MI:0915”(physical association) | 0.600 |
| IP6K2 | MEOX2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RBPMS | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MEOX2 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| IP6K2 | RBPMS | psi-mi:“MI:0915”(physical association) | 0.560 |
| HSP90AA1 | IP6K2 | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| IP6K2 | PGK2 | psi-mi:“MI:0914”(association) | 0.560 |
| PLOD3 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| ZBTB2 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| IP6K2 | PGK2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| IP6K2 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| IP6K2 | CCT6A | psi-mi:“MI:0915”(physical association) | 0.400 |
| IP6K2 | IP6K1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| IP6K2 | psi-mi:“MI:0915”(physical association) | 0.370 | |
| PLSCR1 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| IP6K2 | ZBTB2 | psi-mi:“MI:0915”(physical association) | 0.000 |
| PLOD3 | IP6K2 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (24): IP6K2 (Two-hybrid), IP6K2 (Two-hybrid), GTPBP6 (Affinity Capture-MS), IP6K2 (Two-hybrid), IP6K2 (Affinity Capture-RNA), IP6K2 (Two-hybrid), PGK2 (Affinity Capture-MS), RHOU (Affinity Capture-MS), IP6K2 (Affinity Capture-RNA), IP6K2 (Two-hybrid), PLOD3 (Two-hybrid), ZBTB2 (Two-hybrid), IP6K2 (Proximity Label-MS), IP6K2 (Affinity Capture-RNA), PGK2 (Affinity Capture-MS)
ESM2 similar proteins: A7MBL8, B3EX61, G3V7Q0, O00763, O02810, O13010, O60942, O70172, O88370, O88377, O94806, P10687, P10894, P48426, P69341, P78356, P97789, Q0P5F7, Q13613, Q15139, Q15147, Q5F356, Q5PQ01, Q5R488, Q6DIX1, Q6GL14, Q6IQ26, Q6IQE1, Q6PAL8, Q7TT16, Q80V72, Q80XI4, Q8BKC8, Q8BPM2, Q8BWW9, Q8IZH2, Q8K1Y2, Q8NFU5, Q8TBX8, Q91XU3
Diamond homologs: O74561, Q12494, Q6PD10, Q80V72, Q8BWD2, Q92551, Q95221, Q96PC2, Q9ESM0, Q9R0U1, Q9UHH9, A2X5H5, Q6H545, Q7TT16, Q8NFU5, Q99NI4, Q9US14, P07250
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CSNK2A1 | “down-regulates quantity by destabilization” | IP6K2 | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
55 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 39 |
| Likely benign | 2 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1618 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:48688769:TACAC:T | acceptor_gain | 1.0000 |
| 3:48688770:ACAC:A | acceptor_gain | 1.0000 |
| 3:48688771:CAC:C | acceptor_gain | 1.0000 |
| 3:48688771:CACC:C | acceptor_gain | 1.0000 |
| 3:48688772:AC:A | acceptor_gain | 1.0000 |
| 3:48688772:ACC:A | acceptor_loss | 1.0000 |
| 3:48688773:CCTG:C | acceptor_gain | 1.0000 |
| 3:48688774:C:CC | acceptor_gain | 1.0000 |
| 3:48688775:T:C | acceptor_loss | 1.0000 |
| 3:48689701:A:T | acceptor_gain | 1.0000 |
| 3:48691310:A:AC | donor_gain | 1.0000 |
| 3:48691311:C:CC | donor_gain | 1.0000 |
| 3:48691483:C:CC | acceptor_gain | 1.0000 |
| 3:48692949:CTCA:C | donor_loss | 1.0000 |
| 3:48692950:TCACC:T | donor_loss | 1.0000 |
| 3:48692951:CACCT:C | donor_loss | 1.0000 |
| 3:48692952:ACC:A | donor_loss | 1.0000 |
| 3:48692953:CCT:C | donor_gain | 1.0000 |
| 3:48693177:CAC:C | acceptor_gain | 1.0000 |
| 3:48693178:ACCT:A | acceptor_loss | 1.0000 |
| 3:48693180:C:CC | acceptor_gain | 1.0000 |
| 3:48693180:CTGGA:C | acceptor_loss | 1.0000 |
| 3:48693190:G:C | acceptor_gain | 1.0000 |
| 3:48695085:CTTA:C | donor_loss | 1.0000 |
| 3:48695086:TTA:T | donor_loss | 1.0000 |
| 3:48695087:TA:T | donor_loss | 1.0000 |
| 3:48695088:A:AC | donor_gain | 1.0000 |
| 3:48695089:C:CC | donor_gain | 1.0000 |
| 3:48695089:C:CT | donor_loss | 1.0000 |
| 3:48695417:CTCTG:C | acceptor_gain | 1.0000 |
AlphaMissense
2819 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:48688316:A:G | L413P | 1.000 |
| 3:48688325:A:G | L410P | 1.000 |
| 3:48688328:C:T | G409E | 1.000 |
| 3:48688329:C:A | G409W | 1.000 |
| 3:48688329:C:G | G409R | 1.000 |
| 3:48688329:C:T | G409R | 1.000 |
| 3:48688347:C:G | D403H | 1.000 |
| 3:48688402:A:C | F384L | 1.000 |
| 3:48688402:A:T | F384L | 1.000 |
| 3:48688404:A:G | F384L | 1.000 |
| 3:48688405:G:C | D383E | 1.000 |
| 3:48688405:G:T | D383E | 1.000 |
| 3:48688406:T:A | D383V | 1.000 |
| 3:48688406:T:C | D383G | 1.000 |
| 3:48688406:T:G | D383A | 1.000 |
| 3:48688407:C:G | D383H | 1.000 |
| 3:48688415:C:G | R380P | 1.000 |
| 3:48688559:A:G | L332P | 1.000 |
| 3:48688562:A:G | L331P | 1.000 |
| 3:48688567:G:C | S329R | 1.000 |
| 3:48688567:G:T | S329R | 1.000 |
| 3:48688569:T:G | S329R | 1.000 |
| 3:48688580:C:G | R325P | 1.000 |
| 3:48688581:G:T | R325S | 1.000 |
| 3:48688613:A:G | L314P | 1.000 |
| 3:48688622:A:G | L311P | 1.000 |
| 3:48688678:G:C | F292L | 1.000 |
| 3:48688678:G:T | F292L | 1.000 |
| 3:48688680:A:G | F292L | 1.000 |
| 3:48688721:C:G | R278P | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000036948 (3:48711108 G>A), RS1000107236 (3:48704045 T>C), RS1000149928 (3:48717731 G>A,T), RS1000227203 (3:48716040 T>C), RS1000475268 (3:48689559 A>G), RS1000594149 (3:48712359 C>T), RS1000608125 (3:48718083 G>A), RS1000744442 (3:48706266 C>T), RS1000764700 (3:48689935 G>A), RS1000802885 (3:48706616 G>C), RS1000865690 (3:48705304 G>A), RS1000893090 (3:48702661 G>GTGT), RS1000943169 (3:48716794 G>A), RS1000957470 (3:48693615 G>A,C), RS1001046407 (3:48712656 T>C)
Disease associations
OMIM: gene MIM:606992 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
28 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001725_77 | Inflammatory bowel disease | 1.000000e-47 |
| GCST002548_9 | Ulcerative colitis | 8.000000e-07 |
| GCST002774_5 | Cognitive function | 3.000000e-06 |
| GCST004131_23 | Inflammatory bowel disease | 1.000000e-33 |
| GCST004132_17 | Crohn’s disease | 3.000000e-23 |
| GCST004133_11 | Ulcerative colitis | 8.000000e-20 |
| GCST006269_813 | General cognitive ability | 9.000000e-09 |
| GCST006611_70 | HDL cholesterol | 7.000000e-09 |
| GCST006944_33 | Experiencing mood swings | 4.000000e-09 |
| GCST006947_44 | Feeling fed-up | 1.000000e-10 |
| GCST007094_111 | Diastolic blood pressure | 2.000000e-08 |
| GCST007565_146 | Morning person | 6.000000e-17 |
| GCST009325_92 | Parkinson’s disease or first degree relation to individual with Parkinson’s disease | 1.000000e-10 |
| GCST009524_287 | Household income (MTAG) | 4.000000e-09 |
| GCST009524_340 | Household income (MTAG) | 6.000000e-13 |
| GCST010002_422 | Refractive error | 4.000000e-14 |
| GCST010698_80 | Subcortical volume (min-P) | 3.000000e-24 |
| GCST010699_110 | Brain morphology (min-P) | 4.000000e-08 |
| GCST010701_52 | Cortical surface area (MOSTest) | 1.000000e-16 |
| GCST010702_36 | Subcortical volume (MOSTest) | 1.000000e-10 |
| GCST010703_262 | Brain morphology (MOSTest) | 2.000000e-13 |
| GCST010988_141 | Adult body size | 7.000000e-14 |
| GCST012226_606 | Waist circumference adjusted for body mass index | 3.000000e-12 |
| GCST012226_608 | Waist circumference adjusted for body mass index | 8.000000e-09 |
| GCST012232_6 | Lipoprotein (a) levels | 5.000000e-09 |
| GCST90000050_21 | Age at first birth | 9.000000e-19 |
| GCST90002381_148 | Eosinophil count | 1.000000e-13 |
| GCST90020029_1174 | Waist circumference adjusted for body mass index | 1.000000e-08 |
EFO canonical traits (12, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004337 | intelligence |
| EFO:0004612 | high density lipoprotein cholesterol measurement |
| EFO:0008475 | mood instability measurement |
| EFO:0009588 | feeling “fed-up” measurement |
| EFO:0006336 | diastolic blood pressure |
| EFO:0008328 | chronotype measurement |
| EFO:0009695 | household income |
| EFO:0004346 | neuroimaging measurement |
| EFO:0007789 | BMI-adjusted waist circumference |
| EFO:0006925 | lipoprotein A measurement |
| EFO:0009101 | age at first birth measurement |
| EFO:0004842 | eosinophil count |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4523488 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 124,022 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL151 | LUTEOLIN | 2 | 23,523 |
| CHEMBL150 | KAEMPFEROL | 1 | 25,940 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
2 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs3172494 | IP6K2 | 0.00 | 0 | ||
| rs61740999 | IP6K2 | 0.00 | 0 |
ChEMBL bioactivities
49 potent at pChembl≥5 of 62 total, top 49 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.31 | IC50 | 4.9 | nM | CHEMBL5190343 |
| 7.60 | IC50 | 25 | nM | CHEMBL5203174 |
| 7.27 | IC50 | 54 | nM | CHEMBL5169462 |
| 7.19 | IC50 | 65 | nM | CHEMBL5186210 |
| 7.15 | IC50 | 71 | nM | CHEMBL5200214 |
| 7.13 | IC50 | 74 | nM | CHEMBL5181623 |
| 7.13 | Kd | 74 | nM | CHEMBL5190343 |
| 7.03 | IC50 | 94 | nM | CHEMBL5184960 |
| 7.03 | IC50 | 94 | nM | CHEMBL5190343 |
| 7.00 | IC50 | 100 | nM | CHEMBL5204881 |
| 6.89 | IC50 | 130 | nM | CHEMBL5184940 |
| 6.89 | IC50 | 130 | nM | CHEMBL5196483 |
| 6.82 | IC50 | 150 | nM | CHEMBL5201078 |
| 6.82 | IC50 | 150 | nM | CHEMBL5186729 |
| 6.72 | IC50 | 190 | nM | CHEMBL5197626 |
| 6.62 | IC50 | 240 | nM | CHEMBL5175579 |
| 6.55 | IC50 | 280 | nM | CHEMBL1460920 |
| 6.55 | IC50 | 280 | nM | CHEMBL5185725 |
| 6.54 | IC50 | 290 | nM | CHEMBL5190846 |
| 6.50 | IC50 | 320 | nM | CHEMBL5201056 |
| 6.46 | IC50 | 350 | nM | CHEMBL5198845 |
| 6.39 | IC50 | 410 | nM | CHEMBL5189856 |
| 6.36 | IC50 | 440 | nM | CHEMBL1379963 |
| 6.32 | IC50 | 480 | nM | CHEMBL5188320 |
| 6.30 | IC50 | 500 | nM | ISORHAMNETIN |
| 6.24 | IC50 | 580 | nM | CHEMBL1485263 |
| 6.24 | IC50 | 580 | nM | CHEMBL5171388 |
| 6.19 | IC50 | 650 | nM | CHEMBL5192487 |
| 6.16 | IC50 | 700 | nM | MYRICETIN |
| 6.16 | IC50 | 700 | nM | QUERCETIN |
| 6.16 | IC50 | 690 | nM | CHEMBL5203362 |
| 6.14 | IC50 | 720 | nM | CHEMBL5185229 |
| 6.09 | IC50 | 820 | nM | CHEMBL5206215 |
| 6.05 | IC50 | 900 | nM | DIOSMETIN |
| 5.92 | IC50 | 1190 | nM | CHEMBL5195827 |
| 5.89 | IC50 | 1300 | nM | LUTEOLIN |
| 5.84 | IC50 | 1460 | nM | CHEMBL5205377 |
| 5.80 | IC50 | 1580 | nM | CHEMBL5178065 |
| 5.75 | IC50 | 1800 | nM | RHAMNETIN |
| 5.70 | IC50 | 2000 | nM | CHEMBL467591 |
| 5.67 | IC50 | 2120 | nM | CHEMBL5209246 |
| 5.62 | IC50 | 2390 | nM | CHEMBL5178548 |
| 5.60 | IC50 | 2500 | nM | KAEMPFEROL |
| 5.31 | Ki | 4880 | nM | CHEMBL4555782 |
| 5.24 | IC50 | 5700 | nM | ACACETIN |
| 5.19 | IC50 | 6510 | nM | CHEMBL5199101 |
| 5.15 | IC50 | 7100 | nM | APIGENIN |
| 5.10 | IC50 | 8000 | nM | CHEMBL243677 |
| 5.06 | IC50 | 8650 | nM | CHEMBL1368139 |
PubChem BioAssay actives
49 with measured affinity, of 89 total; 47 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 3-(4-phenylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909478: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inhibition of [3H]-InsP6 phosphorylation measured after 180 mins by HPLC analysis | ic50 | 0.0049 | uM |
| 1’-(4-chlorobenzoyl)-2-oxospiro[1H-indole-3,4’-piperidine]-5-carboxylic acid | 1909472: Inhibition of recombinant full length human IP6K2 assessed as inorganic phosphate release measured after 30 mins by ADP-Glo Max assay | ic50 | 0.0250 | uM |
| 3-(4-pyridin-3-ylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.0540 | uM |
| 3-(4-benzylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.0650 | uM |
| 3-[3-[(3,5-dichloro-2-pyridinyl)oxy]phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.0710 | uM |
| (E)-3-[3-(4-phenylphenyl)-2,1-benzoxazol-5-yl]prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.0740 | uM |
| (E)-3-[3-(4-phenoxyphenyl)-2,1-benzoxazol-5-yl]prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.0940 | uM |
| 3-(3,5-dimethylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1000 | uM |
| 3-(3-phenylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1300 | uM |
| 3-(3-phenoxyphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1300 | uM |
| 3-(3-methylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1500 | uM |
| 3-(4-pyridin-4-ylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1500 | uM |
| 3-[4-(cyclopentanecarbonylamino)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.1900 | uM |
| 3-(4-piperidin-1-ylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.2400 | uM |
| 3-(4-phenoxyphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.2800 | uM |
| 3-phenyl-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.2800 | uM |
| (E)-3-[3-(3-methylphenyl)-2,1-benzoxazol-5-yl]prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.2900 | uM |
| (E)-3-[3-[4-(trifluoromethoxy)phenyl]-2,1-benzoxazol-5-yl]prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.3200 | uM |
| 3-[4-(propan-2-ylcarbamoyl)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.3500 | uM |
| 3-[3-(cyclopropanecarbonylamino)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.4100 | uM |
| 3-(4-methylphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.4400 | uM |
| 3-[4-(2-oxopyrrolidin-1-yl)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.4800 | uM |
| 3,5,7-trihydroxy-2-(4-hydroxy-3-methoxyphenyl)chromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 0.5000 | uM |
| 3-(4-benzamidophenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.5800 | uM |
| (E)-3-(3-phenyl-2,1-benzoxazol-6-yl)prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.5800 | uM |
| 3-[4-[(3,5-dichloro-2-pyridinyl)oxy]phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.6500 | uM |
| 3-(3-pyridin-2-yloxyphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.6900 | uM |
| Quercetin | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 0.7000 | uM |
| 3,5,7-trihydroxy-2-(3,4,5-trihydroxyphenyl)chromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 0.7000 | uM |
| 3-[4-(pyrimidine-4-carbonylamino)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.7200 | uM |
| 3-[4-(2-methylpropanoylamino)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 0.8200 | uM |
| Diosmetin | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 0.9000 | uM |
| 3-(4-pyridin-2-yloxyphenyl)-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 1.1900 | uM |
| 2-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 1.3000 | uM |
| 3-[3-(trifluoromethyl)phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 1.4600 | uM |
| methyl (E)-3-(3-phenyl-2,1-benzoxazol-5-yl)prop-2-enoate | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 1.5800 | uM |
| 2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxychromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 1.8000 | uM |
| 6-N-[(4-nitrophenyl)methyl]-2-N-[[3-(trifluoromethyl)phenyl]methyl]-7H-purine-2,6-diamine | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 2.0000 | uM |
| N-methyl-3-phenyl-2,1-benzoxazole-5-carboxamide | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 2.1200 | uM |
| 3-[4-[(6-oxopiperidine-3-carbonyl)amino]phenyl]-2,1-benzoxazole-5-carboxylic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 2.3900 | uM |
| 3,5,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 2.5000 | uM |
| 5-[[[2-[2-(6-methoxy-1H-indol-3-yl)ethylamino]-7H-purin-6-yl]amino]methyl]-1H-pyridin-2-one | 1601029: Inhibition of IP6K2 (unknown origin) in presence of ATP at Km concentration by Cheng-Prusoff equation analysis | ki | 4.8800 | uM |
| 5,7-dihydroxy-2-(4-methoxyphenyl)chromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 5.7000 | uM |
| (E)-3-[3-(4-methylphenyl)-2,1-benzoxazol-5-yl]prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 6.5100 | uM |
| 5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 7.1000 | uM |
| 2-(3,4-dihydroxyphenyl)-5-hydroxychromen-4-one | 1572024: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | ic50 | 8.0000 | uM |
| (E)-3-(3-phenyl-2,1-benzoxazol-5-yl)prop-2-enoic acid | 1909469: Inhibition of N-terminal 6His-tagged/TEV cleavage site fused recombinant human IP6K2 expressed in Escherichia coli assessed as inorganic phosphate release using InsP6 as substrate in presence of ATP measured after 60 to 120 mins by malachite green based colorimetric - DIPP1 coupled enzyme assay | ic50 | 8.6500 | uM |
CTD chemical–gene interactions
47 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects expression, decreases expression, decreases methylation | 4 |
| Arsenic | increases abundance, affects methylation, affects cotreatment, increases expression, decreases expression | 3 |
| Estradiol | affects expression, decreases expression | 3 |
| aristolochic acid I | increases expression | 1 |
| 3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | affects expression | 1 |
| beta-lapachone | increases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| sodium arsenite | decreases expression, increases abundance | 1 |
| cobaltous chloride | increases expression | 1 |
| potassium chromate(VI) | affects cotreatment, increases expression | 1 |
| 2,3-bis(3’-hydroxybenzyl)butyrolactone | affects cotreatment, decreases expression | 1 |
| beta-methylcholine | affects expression | 1 |
| epigallocatechin gallate | increases expression, affects cotreatment | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| ICG 001 | decreases expression | 1 |
| abrine | increases expression | 1 |
| Grape Seed Proanthocyanidins | affects cotreatment, decreases expression | 1 |
| 2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine | increases expression, increases response to substance | 1 |
| bisphenol S | increases methylation | 1 |
| PCI 5002 | affects cotreatment, increases expression | 1 |
| Air Pollutants | decreases expression | 1 |
| Catechin | affects cotreatment, decreases expression | 1 |
| Coumestrol | decreases expression, affects cotreatment | 1 |
| Dichlorodiphenyl Dichloroethylene | decreases expression | 1 |
| Ethyl Methanesulfonate | increases expression | 1 |
| Formaldehyde | increases expression | 1 |
| Gallic Acid | increases expression | 1 |
| Iron | affects cotreatment, increases expression | 1 |
ChEMBL screening assays
16 unique, capped per target: 16 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4370053 | Binding | Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay | Inhibition of Inositol Polyphosphate Kinases by Quercetin and Related Flavonoids: A Structure-Activity Analysis. — J Med Chem |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1UL | Abcam HeLa IP6K2 KO | Cancer cell line | Female |
| CVCL_D8NA | Ubigene HCT 116 IP6K2 KO | Cancer cell line | Male |
| CVCL_E0F9 | Ubigene HeLa IP6K2 KO | Cancer cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.