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phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma

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Target id: 2288

Nomenclature: phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma

Abbreviated Name: C2γ/PIK3C2G

Family: Phosphatidylinositol-4-phosphate 3-kinase family, Phosphatidylinositol kinases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1445 12p12.3 PIK3C2G phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma
Mouse - 1506 6 69.7 cM Pik3c2g phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma
Rat - 1505 4q44 Pik3c2g phosphatidylinositol-4-phosphate 3-kinase, catalytic subunit type 2 gamma
Previous and Unofficial Names Click here for help
phosphoinositide 3-kinase-C2-gamma | PI3K-C2-gamma | phosphatidylinositol-4-phosphate 3-kinase, catalytic subunit type 2 gamma | phosphatidylinositol-4-phosphate 3-kinase | phosphatidylinositol 3-kinase, C2 domain containing, gamma polypeptide
Database Links Click here for help
Alphafold O75747 (Hs), O70167 (Mm), O70173 (Rn)
BRENDA 2.7.1.154
CATH/Gene3D 1.10.1070.11, 2.60.40.150, 3.30.1520.10
ChEMBL Target CHEMBL1163120 (Hs)
Ensembl Gene ENSG00000139144 (Hs), ENSMUSG00000030228 (Mm), ENSRNOG00000034228 (Rn)
Entrez Gene 5288 (Hs), 18705 (Mm), 116720 (Rn)
Human Protein Atlas ENSG00000139144 (Hs)
KEGG Enzyme 2.7.1.154
KEGG Gene hsa:5288 (Hs), mmu:18705 (Mm), rno:116720 (Rn)
OMIM 609001 (Hs)
Pharos O75747 (Hs)
RefSeq Nucleotide NM_004570 (Hs), NM_207683 (Mm), NM_053923 (Rn)
RefSeq Protein NP_004561 (Hs), NP_997566 (Mm), NP_446375 (Rn)
UniProtKB O75747 (Hs), O70167 (Mm), O70173 (Rn)
Wikipedia PIK3C2G (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.1.154

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SAR260301 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.4 pIC50 1
⤷ pIC50 5.4 (IC50 3.812x10-6 M) [1]
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2-3
Key to terms and symbols Click column headers to sort
Target used in screen: PIK3C2G
Ligand Sp. Type Action Value Parameter
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C et al.. (2014) Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J Med Chem, 57 (3): 903-20. [PMID:24387221]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

3. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

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