-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Z-FA-FMK ((1S)-Z-FA-FMK) 是一种有效的组织蛋白酶 B 和 L 抑制剂。Z-FA-FMK 通过选择性合成类维生素 a 相关分子 (RRMs) 阻断 DEVDase 活性、DNA 片段化和磷脂酰丝氨酸外化的诱导。Z-FA-FMK 抑制细胞凋亡 (apoptosis)。Z-FA-FMK 可抑制 caspase 活性,并选择性抑制重组效应蛋白 caspase 2、-3、-6 和 -7。Z-FA-FMK 是一种病毒抑制剂。Z-FA-FMK 抑制呼肠孤病毒在易感宿主中的复制。
生物活性
Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host.
性状
Solid
IC50 & Target[1][2]
Cathepsin B cathepsin L
体外研究(In Vitro)
Z-FA-FMK ((1S)-Z-FA-FMK; 5-100 μM; 1 h; Jurkat cells) reduces levels of DEVDase activity and DNA fragmentation. Z-FA-FMK inhibits the externalization of phosphatidylserine induced by either MX2870-1 or MX781.Z-FA-FMK (100 μM; 1 h; Jurkat cells) inhibits apoptosis. Z-FA-FMK inhibited the induction of DEVDase activity not only by the RRMs but also by other apoptotic insults, including etoposide-, ceramide-, and CD95/Fas receptor-mediated pathways.Z-FA-FMK (0-100 μM; 1 h; Jurkat cells) inhibits caspases 2, -3, -6, and -7 activity through repressed induction of DEVDase activity in Jurkat cells. Z-FA-FMK (0-20 μM; 48 h; HT1080 and mouse embryonic stem cells) blocks reoviral replication and cures cells of a persistent infection with reovirus in vitro.Z-FA-FMK (20 μM; 48 h; HT1080 cells) induces defects in reoviral maturation.
体内研究(In Vivo)
Z-FA-FMK (1 mg/kg; intratumor injection; every 2 d, for 27 d; SCID mice with HT1080 xenograft) blocks reovirus infection in vivo.
Z-FA-FMK (8 mg/kg; i.v.; every 2 d, once; male BALB/c mice) markedly lessens the degree of impairment seen in D-GalN/TNF-α-induced kidney injury. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Lopez-Hernandez FJ, et, al. Z-FA-fmk inhibits effector caspases but not initiator caspases 8 and 10, and demonstrates that novel anticancer retinoid-related molecules induce apoptosis via the intrinsic pathway. Mol Cancer Ther. 2003 Mar;2(3):255-63.[2]. Kim M, et, al. Z-FA-FMK as a novel potent inhibitor of reovirus pathogenesis and oncolysis in vivo. Antivir Ther. 2010;15(6):897-905.
溶解度数据
In Vitro: DMSO : 250 mg/mL (646.96 mM; Need ultrasonic)配制储备液