BOC-D-FMK

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.

Signaling Pathways >> Apoptosis >> Caspase

Research Areas >> Cancer

Caspase

Apoptosis is a pathway of cell death orchestrated by a family of proteases called caspases. Boc-D-fmk inhibits TNFα-stimulated reactive oxygen species (ROS) generation. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM[1]. BocD-fmk at 50 µM prevents genistein-induced apoptosis of p815 cells. Confocal microscopy shows that the release of mitochondrial apoptotic factors is inhibited by BocD-fmk[2].

Boc-D-FMK-fmk effectively attenuates the hepatocyte apoptosis in bile duct-ligated rats and may improve the survival rates after endotoxin challenge[3]. A single injection of Boc-D-FMK results in longterm protection of MNs against root avulsion-induced death for more than 8 weeks and the Boc-D-FMK-treated MNs are able to regenerate their axons into an implanted PN graft and reinnervate the target muscle[4].

Rats: Boc-D-FMK is dissolved in DMSO. Male Sprague-Dawley rats group 1 (OBBOC-D) undergo common bile duct ligation and simultaneously treatment with Boc-D-FMK. The first dose of Boc-D-FMK (1.5 mg/kg) is injected into the inferior vena cava immediately after bile duct ligation. Subsequent doses of Boc-DFMK (1.5 mg/kg twice daily) are given intraperitoneally on the first and second postoperative days. The last dose (1.5 mg/kg) is given on the morning of the third postoperative day[3].

[1]. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species.

[2]. Yee SB, et al. zVAD-fmk, unlike BocD-fmk, does not inhibit caspase-6 acting on 14-3-3/Bad pathway in apoptosis of p815 mastocytoma cells. Exp Mol Med. 2006 Dec 31;38(6):634-42.

[3]. Sheen-Chen SM, et al. Effect of Boc-D-Fmk on hepatocyte apoptosis after bile duct ligation in rat and survival rate after endotoxin challenge. J Gastroenterol Hepatol. 2008 Aug;23(8 Pt 1):1276-9.

[4]. Chan YM, et al. Inhibition of caspases promotes long-term survival and reinnervation by axotomized spinal motoneurons of denervated muscle in newborn rats. Exp Neurol. 2003 Jun;181(2):190-203.

Z-VAD(OMe)-FMK | VX-765 | QVD-OPh | Z-DEVD-FMK | Z-IETD-FMK | Sodium tauroursodeoxycholate | Ac-DEVD-CHO | Emricasan | PAC-1 | Taurochenodeoxycholic acid | 20(S)-Ginsenoside Rh2 | 2-HBA | Biotin-VAD-FMK | EP1013 | Ginsenoside Rh4