WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406636
Description: VPS34-IN1 is a potent and selective Vps34 inhibitor with potential anticancer activity. VPS34-IN1 inhibits Vps34 with 25 nM IC50 in vitro, but does not significantly inhibit the activity of 340 protein kinases or 25 lipid kinases tested that include all isoforms of class I as well as class II PI3Ks. Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1 min, without affecting the ability of class I PI3K to regulate Akt. Combining class I (GDC-0941) and class III (VPS34-IN1) PI3K inhibitors could be used as a strategy to better analyse the roles and regulation of the elusive class II PI3K.
MedKoo Cat#: 406636
Chemical Formula: C21H24ClN7O
Exact Mass: 425.17309
Molecular Weight: 425.91
Elemental Analysis: C, 59.22; H, 5.68; Cl, 8.32; N, 23.02; O, 3.76
Synonym: VPS34IN1, VPS34 IN1, VPS34-IN1
IUPAC/Chemical Name: 1-((2-((2-chloropyridin-4-yl)amino)-4'-(cyclopropylmethyl)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol
InChi Key: AWNXKZVIZARMME-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H24ClN7O/c1-21(2,30)12-26-19-25-11-15(17(29-19)9-13-3-4-13)16-6-8-24-20(28-16)27-14-5-7-23-18(22)10-14/h5-8,10-11,13,30H,3-4,9,12H2,1-2H3,(H,25,26,29)(H,23,24,27,28)
SMILES Code: OC(C)(C)CNC(N=C1CC2CC2)=NC=C1C3=CC=NC(NC4=CC=NC(Cl)=C4)=N3
1: Bilanges B, Vanhaesebroeck B. Cinderella finds her shoe: the first Vps34 inhibitor uncovers a new PI3K-AGC protein kinase connection. Biochem J. 2014 Dec 1;464(2):e7-10. doi: 10.1042/BJ20141218. PubMed PMID: 25395352.
2: Bago R, Malik N, Munson MJ, Prescott AR, Davies P, Sommer E, Shpiro N, Ward R, Cross D, Ganley IG, Alessi DR. Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase. Biochem J. 2014 Nov 1;463(3):413-27. doi: 10.1042/BJ20140889. PubMed PMID: 25177796; PubMed Central PMCID: PMC4209782.