|N-ALPHA-[(苄氧基)羰基]-N-(4-氟-3-氧代-2-丁烷基)苯丙氨酰胺|CsnPharm

CAS No.: 197855-65-5

Z-FA-FMK Catalog No. CSN12249

Synonyms: (1S)-Z-FA-FMK;Z-Phe-Ala-Fluoromethyl Ketone;Z-FA-fluoromethyl ketone

Z-FA-FMK is an irreversible cysteine protease inhibitor,which also inhibits effector caspases.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Z-FA-FMK is an irreversible inhibitor of cathepsin B, including cathepsins B and L, and also inhibits DEVDase caspase activity. Preincubation with Z-FA-FMK could dose-dependently inhibit activation of caspase at concentration of 30, 60 and 150μM in HeLa cell extracts. The activity inhibition of caspase 2, 3, 6, 7 and 9 could be observed. Pre-treatment with 100μM Z-FA-fmk for 1h could inhibit the induction of DEVDase activity by stimuli in intact Jurkat cells, but without cytochrome c release. Pre-treatment with Z-FA-fmk at concentration ranging in 10-100μM for 2h dose-dependently inhibited processing and activation of caspase-2, 3, 7 and 9, as well as cleavage of Bid, induced by treatment with 1μM MX2870-1 for 3h. Z-FA-FMK could partially inhibit the activity of mature effector caspases in intact cells at low concentration and prevent the cleavage and activation of effector caspases initiated by caspase 9 correlating with partial inhibition of mature caspase 9 at higher concentrations^[1]. Z-FA-FMK is immunosuppressive in vitro and in vivo. Z-FA-FMK inhibited IL-2-driven T cell proliferation by preventing cells from entering and leaving the cell cycle, and inhibited the IL-2 autocrine system in T lymphocytes at concentration of 100μM. The inhibition of translocation of cellular p65 to the nucleus by z-FA-FMK could be observed in purified T cells costimulated with anti-CD3 and anti-CD28. Z-FA-FMK inhibited the processing of caspase-8 and caspase-3 to their respective subunits in resting T cells stimulated through the Ag receptor but not during Fas-induced apoptosis in proliferating T cells. Administration of 25mg/kg, i.v., increased pneumococcal load in the blood and lungs of MFI mice^[2].
作用机制Z-FA-fmk can bind to purified caspase.^[1]
动物研究
剂量
Mice^[3] (i.v.): 8 mg/kg

给药途径
i.v.
参考文献

动物研究
剂量	Mice^[3] (i.v.): 8 mg/kg
给药途径	i.v.

[1] Lopez-Hernandez FJ, Ortiz MA, 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] Lawrence CP, Kadioglu A, et al. The cathepsin B inhibitor, z-FA-FMK, inhibits human T cell proliferation in vitro and modulates host response to pneumococcal infection in vivo. J Immunol. 2006 Sep 15;177(6):3827-36.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5879 mL
- 12.9394 mL
- 25.8788 mL
- 5 mM
- 0.5176 mL
- 2.5879 mL
- 5.1758 mL
- 10 mM
- 0.2588 mL
- 1.2939 mL
- 2.5879 mL

技术信息

CAS号

197855-65-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23FN2O4

运输

蓝冰

分子量

386.42

别名

(1S)-Z-FA-FMK;Z-Phe-Ala-Fluoromethyl Ketone;Z-FA-fluoromethyl ketone

溶解度

DMSO	360.0 mg/mL (931.6 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Z-FA-FMK Catalog No. CSN12249

靶点选择性

请登录您的专属账户

确认信息