Z-YVAD-FMK

AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

Caspase

Z-YVAD-FMK (100 μM; 24 hours) significantly downregulated the growth inhibition induced by butyrate in Caco-2 cells[1]. Z-YVAD-FMK (20 μM; pre 1 hour; 24 hours) attenuates the apoptotic induction of III-10 on both HepG2 and BEL-7402 cells, the apoptotic rate of -10 on HepG2 cells is reduced by Z-VAD-FMK from 19.88% to 8.34%, while that on BEL-7402 cells is reduced from 17.56% to 11.98%[4]. Z-YVAD-FMK (1-10 μM; 24 hours) shows inhibitory effect in various cells against TNFr- or anti-CD95-induced cell death, exhibits IC50 values of 0.0015 μM (Murine hepatocytes), 0.027 μM (Murine hepatocytes), 4.8 μM (HepG2), 5.8 μM (HepG2), 1.6 μM (Hela) and 1.1 μM (Jurkat), respectively[5]. Cell Viability Assay[1] Cell Line: Caco-2 cells Concentration: 0-100 μM Incubation Time: 24 hours Result: Inhibited Caco-2 cells growth. Apoptosis Analysis[1] Cell Line: BEL-7402 and HepG2 cells Concentration: 20 μM Incubation Time: Pre 1 hour; 24 hours Result: Induced a caspase-dependent apoptosis in cells.

Z-VAD-FMK (intraperitoneal injection; 10mg/kg; pre- 30 minutes) significantly delayed preterm delivery at 18 hours, but after 36 hours treatment, non different exists between Z-VAD-FMK-pretreated and control groups[3]. Animal Model: Day 14.5 pregnant CD1 mice[3] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10mg/kg; pre-30 minutes Result: Prevented HK-GBS-induced preterm delivery.

[1]. Li H1,et al.Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1beta and IL-18 release.J Immunol. 2007 Apr 15;178(8):5271-6.

[2]. Avivi-Green C, et al. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines.J Nutr. 2002 Jul;132(7):1812-8.

[3]. Equils O, et al. Pretreatment with pancaspase inhibitor (Z-VAD-FMK) delays but does not prevent intraperitoneal heat-killed group B Streptococcus-induced preterm delivery in a pregnant mouse model.infect Dis Obstet Gynecol. 2009;2009:749432.

[4]. Künstle G,et al. ICE-protease inhibitors block murine liver injury and apoptosis caused by CD95 or by TNF-alpha.Immunol Lett. 1997 Jan;55(1):5-10.