Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

METHODS: Neutrophils were treated with Z-VAD-FMK (0.03-300 µM) for 30 min, then incubated with 200 U/mL TNFα for 6 h. Apoptosis was detected by Flow Cytometry.
RESULTS: Z-VAD-FMK had a biphasic effect on TNFα-stimulated neutrophil apoptosis. 100 µM or more of Z-VAD-FMK enhanced TNFα-induced apoptosis, whereas 30 µM or less inhibited apoptosis. [1]
METHODS: Human colorectal cancer cells HCT116 and SW480 were pretreated with Z-VAD-FMK (20 μM) for 1 h, then incubated with CPT (10-1000 ng/mL) and 5-FU (5-12.5 μg/mL) for 48 h to induce apoptosis, and then the expression levels of target proteins were detected by Western Blot.
RESULTS: CPT and 5-FU induced significant up-regulation of cleaved caspase-3, caspase-8 and PARP, and Z-VAD-FMK pretreatment eliminated the activation of apoptosis-related proteins. [2]
METHODS: Human T-lymphoblastic leukemia cells Jurkat were treated with Z-VAD-FMK (10-200 µM) for 24 h after pulsing, and cell viability was measured using propidium iodide.
RESULTS: The optimal concentration of Z-VAD-FMK was 50 µM, which increased cell viability from 35% to 74% compared to untreated control. [3]

METHODS: To detect anti-tumor activity in vivo, C57/BL6 mice bearing mouse melanoma tumor B16 were treated with RT (2 Gy local irradiation of the tumor on day 8/9/10), DTIC (2 mg/pc intraperitoneal injection on day 8/10), and a combination of Z-VAD-FMK (2 mg/kg intraperitoneal injection on day 8/9/10) and HT (4 h post-irradiation on day 8/10).
RESULTS: Multimodal tumor therapy with RT, DTIC, and HT in combination with Z-VAD-FMK retarded tumor growth in a T-cell-dependent manner. [4]
METHODS: To investigate the role of Z-VAD-FMK in endotoxin shock, Z-VAD-FMK (5-20 μg/g) was administered as a single intraperitoneal injection to LPS-induced endotoxin shock in C57BL/6 mice.
RESULTS: Z-VAD-FMK treatment significantly prolonged the survival time of mice for several hours and increased the survival rate. Z-VAD-FMK treatment significantly reduced the mortality rate of mice treated with different doses of LPS. [5]