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

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

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma in GtoImmuPdb

Gene and Protein Information
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 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
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
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.1.154

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 28 [PMID: 24387221] Hs Inhibition 5.4 pIC50 1
pIC50 5.4 (IC50 3.812x10-6 M) [1]
DiscoveRx KINOMEscan® screen
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 Affinity Units
TG-100-115 Hs Inhibitor Inhibition 8.5 pKd
PI-103 Hs Inhibitor Inhibition 7.4 pKd
PP-242 Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Hs Inhibitor Inhibition 6.6 pKd
pictilisib Hs Inhibitor Inhibition 6.5 pKd
staurosporine Hs Inhibitor Inhibition 6.4 pKd
midostaurin Hs Inhibitor Inhibition 6.2 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib 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]

How to cite this page

Phosphatidylinositol kinases: phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma. Last modified on 29/01/2016. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2288.