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Z-FA-FMK

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Chemical Structure| 197855-65-5 同义名 : (1S)-Z-FA-FMK;Z-Phe-Ala-Fluoromethyl Ketone;Z-FA-fluoromethyl ketone
CAS号 : 197855-65-5
货号 : A444845
分子式 : C21H23FN2O4
纯度 : 99%+
分子量 : 386.417
MDL号 : MFCD02684535
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(646.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Cysteine Protease
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.88mL

5.18mL

2.59mL
参考文献

[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.