Wortmannin

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity; inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release up to 80% with IC50 of 2.0 and 3.0 nM, respectively; Also inhibits DNA-PK and MLCK. (In Vitro) :Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively. Wortmannin prevents nuclear entry of YAP. (In Vivo) :Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation.

19545-26-7

SL-2052 | KY-12420

>98% (HPLC)

10 mM in DMSO

CC (O[C@@H] (C1=C2C (C3=C4C (C (O[C@H] (COC) [C@]14C) =O) =CO3) =O) C[C@]5 (C) C (CC[C@]52[H]) =O) =O

C23H24O8

428.4319

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.