A-443654

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBalpha, beta, gamma) modulate cell proliferation, metabolism, and survival as well as angiogenesis. A-443654 is an inhibitor of Akt (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation. It induces G2/M accumulation, defects in centrosome separation, and formation of either monopolar arrays or disorganized spindles. A-443654 has been reported to slow the progression of Akt-dependent tumors in in vivo mouse models. In response to an A-443654-induced decrease in phosphorylation of Akt targets, a concomitant increase in Thr308 and Ser473 phosphorylation of Akt has been observed in human cancer cell lines. A-443654 has been used to examine the mechanism of this rapid feedback reaction.Formal Name: alphaS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-1H-indole-3-ethanamine. CAS Number: 552325-16-3. Molecular Formula: C24H23N5O. Formula Weight: 397.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 15 mg/ml, Ethanol: 10 mg/ml. lambdamax: 222, 291 nm. SMILES: N[C@@H](CC1=CNC2=C1C=CC=C2)COC3=CC(C4=CC(C(C)=NN5)=C5C=C4)=CN=C3. InChi Code: InChI=1S/C24H23N5O/c1-15-22-10-16(6-7-24(22)29-28-15)17-9-20(13-26-11-17)30-14-19(25)8-18-12-27-23-5-3-2-4-21(18)23/h2-7,9-13,19,27H,8,14,25H2,1H3,(H,28,29)/t19-/m0/s1. InChi Key: YWTBGJGMTBHQTM-IBGZPJMESA-N.