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Description

A Torin1 (Cat. No. 475991) structural analog that acts as a cell-permeable, potent, ATP-competitive inhibitor against DNA-PK and mTOR (IC50 = 0.5 and 2.81 nM, respectively). Comparing to Torin1, Torin2 displays enhanced inhibitory potency against PI 4-Kbeta (IC50 = 18.3 nM) and PI 3-K (IC50 =4.68, 5.67, 8.58, 17.5, 24.5, and 28.1 nM, respectively, against P110alpha/P85alpha, P110gamma, hVPS34, P110delta/P85alpha, C2beta, C2alpha, respectively), while being more effective in inhibiting S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 0.25 nM vs 2 nM, respectively, for Torin2 and Torin1) in vitro and displaying much improved oral bioavailability in mice (Cmax (ng/mL) /T1/2 (h) = 3968/0.72 and 223/0.79, respectively, for Torin2 and Torin1, 10 /mg/kg p.o.) in vivo.