533557 Sigma-AldrichAKT Inhibitor XXIII, Isozyme-Selective, GSK2141795 - CAS 1047634-65-0 - Calbiochem

This product has been discontinued.

A cell-permeable, orally available, and non-toxic pyrazolylfuran-carboxamide derived compound that acts as a highly potent, ATP-competitive, and reversible inhibitor of Akt1, Akt2, Akt3 (IC₅₀ = 66 pM, 1.4 nM, and 1.5 nM, respectively). Shown to block the phosphorylation of multiple Akt substrates. Also shown to be a highly effective inhibitor of E17K mutant form of Akt1 (IC₅₀ = 200 pM). Inhibits the activity of PKA, PKG1α, and PKG1β (IC₅₀ = 2, <1, and <1 nM, respectively), but shows high selectivity over a wide panel of other protein kinases. Modestly inhibits several PKC isozymes at much higher concentrations (IC₅₀ = 90 nM). Induces cell cycle arrest at G1 phase and causes apoptosis in BT474, LNCaP, A3, and 19.2 cell lines (~ 1 µM). Suppresses the growth of BT474 xenograft tumors in mice (98% at 30 mg/kg; 57% at 20 mg/kg, p.o. q.d x 21 days). Also induces a transient increase in blood glucose and corresponding insulin levels (200 mg/dl and 188 ng/ml, respectively with a single dose of 30 mg/kg).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.