A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20nM), and p70S6K (IC50 = 85nM) in an ATP-competitive manner (Ki = 18nM using AKT2), with much reduced potency toward RSK1 (IC50 >100nM) and a panel of 13 other cellular kinases (IC50 >1uM). Shown to reduce cellular phosphorylation of GSK-3beta (IC50 range from 2.08 to 4.45uM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86uM) and in mice in vivo (20mg/kg via i.p. or 90mg/kg via p.o.).
Synonyms:p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
Molecular Formula:C₂₀H₂₀ClN₃
Solubility:DMSO
Molar Mass:337.9
Storage and Stability:Store at 4°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
