CCT128930

• CAT Number: I005317
• CAS Number: 885499-61-6
• Molecular Formula: C18H20ClN5
• Molecular Weight: 341.8
• Purity: ≥95%
• Target: Akt
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.6 nM
• InChI: InChI=1S/C18H20ClN5/c19-14-3-1-13(2-4-14)11-18(20)6-9-24(10-7-18)17-15-5-8-21-16(15)22-12-23-17/h1-5,8,12H,6-7,9-11,20H2,(H,21,22,23)
• InChIKey: RZIDZIGAXXNODG-UHFFFAOYSA-N
• SMILES: ClC(C=C1)=CC=C1CC(CC2)(N)CCN2C3=C4C(NC=C4)=NC=N3

CCT128930 (CAT: I005317) is a potent and selective ATP-competitive inhibitor of Akt2, with an IC50 of 6 nM. It exhibits more than 28-fold selectivity for Akt2 compared to the closely related PKA kinase. By inhibiting Akt activity in vitro and in vivo, CCT128930 elicits significant antitumor responses. It demonstrates strong antiproliferative activity and effectively inhibits the phosphorylation of various Akt substrates in multiple tumor cell lines, indicating its ability to block the Akt pathway. In PTEN-null U87MG human glioblastoma cells, CCT128930 induces G1 cell cycle arrest, consistent with its inhibition of the Akt pathway and its potential as a therapeutic agent against cancer.

Reference

1:CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. Wang FZ, Chang ZY, Fei HR, Yang MF, Yang XY, Sun BL.Biochimie. 2014 Aug;103:118-25. doi: 10.1016/j.biochi.2014.04.008. Epub 2014 May 1. PMID: 24793486
2:Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29. PMID: 21191045 Free PMC Article