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

Target id: 2151

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

Abbreviated Name: C2β/PIK3C2B

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 beta in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1634 1q32 PIK3C2B phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta
Mouse - 1632 1 E4 Pik3c2b phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta
Rat - 1621 13 q13 Pik3c2b phosphatidylinositol-4-phosphate 3-kinase
Previous and Unofficial Names
PI3K-C2beta | PtdIns-3-kinase C2 subunit beta | phosphatidylinositol-4-phosphate 3-kinase, catalytic subunit type 2 beta | phosphatidylinositol-4-phosphate 3-kinase
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
PI-103 Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [2]
torin 2 Hs Inhibition 7.6 pIC50 3
pIC50 7.6 (IC50 2.45x10-8 M) [3]
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3C2B
Ligand Sp. Type Action Affinity Units
TG-100-115 Hs Inhibitor Inhibition 8.1 pKd
PI-103 Hs Inhibitor Inhibition 8.0 pKd
pictilisib Hs Inhibitor Inhibition 6.9 pKd
PP-242 Hs Inhibitor Inhibition 6.7 pKd
lapatinib Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Hayakawa M, Kawaguchi K, Kaizawa H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI et al.. (2007) Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg. Med. Chem.15 (17): 5837-44. [PMID:17601739]

3. Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. (2011) Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J. Med. Chem.54 (5): 1473-80. [PMID:21322566]

4. 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 beta. Last modified on 29/01/2016. Accessed on 12/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2151.