M 50054

M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Inflammation/Immunology

M50054 inhibits the caspase-3 activation by Etoposide in a dose-dependent manner. The IC50 value of M50054 against Etoposide-induced caspase-3 activation of U937 cells is 79 μg/mL. However, M50054 does not directly inhibit the enzymatic activity of caspase-3 at all concentrations up to 1000 μg/mL[1]. M50054 (1-300 μg/mL) inhibits soluble human Fas ligand-induced cell death of human Fas-expressing WC8 cells in a dose-dependent manner, and the IC50 of 67 μg/mL[1]. M50054 (30-300 μg/mL) inhibits the death of U937 cells induced by etoposide (10 μg/mL) in a dose-dependent manner, and the IC50 value of M50054 against Etoposide-induced cell death of U937 cells is 130 μg/mL. The IC50 value of M50054 against etoposide-induced DNA fragmentation of U937 cells was 54 μg/mL[1]. Cell Proliferation Assay[1] Cell Line: Human Fas-expressing WC8 cells Concentration: 1, 3, 10, 30, 100, 300 μg/mL Incubation Time: Pre-incubated for 30 min Result: Inhibited soluble human Fas ligand-induced cell death of human Fas-expressing WC8 cells in a dose-dependent manner, and the IC50 of 67 μg/mL.

M50054 (10-300 mg/kg; oral administration 30 min before anti-Fas antibody injection) inhibits the elevation of alanine aminotransferase and aspartate aminotransferase in a dose-dependent manner[1]. M50054 (topical treatment; given daily beginning on day 5 after birth and ending on day 14) significantly improves alopecia (hair loss) symptoms[1]. Animal Model: Female BALB/c mice[1] Dosage: 10, 30, 100 or 300 mg/kg Administration: Orally administered in a volume of 10 mL/kg Result: Inhibited the elevation of alanine aminotransferase and aspartate aminotransferase in a dose-dependent manner. Significantly improved these parameters at doses of 100 mg/kg and 300 mg/kg. Animal Model: Five-day-old SD rats[1] Dosage: Administration: Topically applied to the head and back of 5-day-old rats once daily for 10 days Result: Alopecia scores significantly decreased throughout the entire observation period compared with the control group.

[1]. T Tsuda, et al. Inhibitory effect of M50054, a novel inhibitor of apoptosis, on anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia. Eur J Pharmacol.2001 Dec 14;433(1):37-45.