Top ▲

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

Click here for help

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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1634 1q32.1 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, catalytic subunit type 2 beta
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold O00750 (Hs)
BRENDA 2.7.1.154
CATH/Gene3D 1.10.1070.11, 2.60.40.150, 3.30.1520.10
ChEMBL Target CHEMBL5554 (Hs)
Ensembl Gene ENSG00000133056 (Hs), ENSMUSG00000026447 (Mm), ENSRNOG00000029938 (Rn)
Entrez Gene 5287 (Hs), 240752 (Mm), 289021 (Rn)
Human Protein Atlas ENSG00000133056 (Hs)
KEGG Enzyme 2.7.1.154
KEGG Gene hsa:5287 (Hs), mmu:240752 (Mm), rno:289021 (Rn)
OMIM 602838 (Hs)
Pharos O00750 (Hs)
RefSeq Nucleotide NM_002646 (Hs), NM_001099276 (Mm), NM_001105951 (Rn)
RefSeq Protein NP_002637 (Hs), NP_001092746 (Mm), NP_001099421 (Rn)
UniProtKB O00750 (Hs)
Wikipedia PIK3C2B (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
PI-103 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 2
⤷ pIC50 8.0 (IC50 1x10-8 M) [2]
torin 2 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 3
⤷ pIC50 7.6 (IC50 2.45x10-8 M) [3]
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: 1,4
Key to terms and symbols Click column headers to sort
Target used in screen: PIK3C2B
Ligand Sp. Type Action Value Parameter
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
lapatinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 5.6 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
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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