uprosertib-gsk2141795-hcl

Description: Uprosertib (formerly known as GSK2141795 and GSK795), an analog of GSK2110183, is a potent, orally bioavailable and ATP-competitive Akt inhibitor with IC50 values of 180 nM, 328 nM, and 38 nM for Akt1/Akt2/Akt3, respectively. Uprosertib is an inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor Uprosertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

References: Nat Commun. 2017 Sep 4; 8(1):410. doi: 10.1038/s41467-017-00450-6; J Proteome Res. 2013 Aug 2; 12(8):3792-800; Cancer Chemother Pharmacol. 2015 Jan; 75(1):183-9; Blood. 2014 Oct 2; 124(14):2162-3.

Related CAS #: 1047634-65-0 (Uprosertib free base); 1047634-63-8 (GSK2110183); 1047644-62-1 (Afuresertib / GSK2110183C); 1047645-82-8 (Afuresertib HCl / GSK2110183B)