Wortmannin

19545-26-7

C23H24O8

DMSO : >= 50 mg/mL (116.71 mM)

PI3K/Akt/mTOR; Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Cell Cycle/DNA Damage; Cell Cycle/DNA Damage; PI3K/Akt/mTOR

Wortmannin is a multi-target inhibitor. Wortmannin inhibits PI3K^[1], MLCK^[1], DNA-PK^[2], ATM^[2], ATR^[2], and Polo-like kinase 3 (Plk3^[3]) with IC₅₀s of 3 nM, 200 nM, 16 nM, 150 nM, 1.8 uM and 48 nM, respectively. IC50 & Target: IC50: 3 nM (PI3K), 200 nM (MLCK)^[1]
IC50: 16 nM (DNA-PK), 150 nM (ATM), 1.8 uM (ATR)^[2] 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^[4]. 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^[5].