Z-FA-FMK
(Synonyms: 半胱氨酸蛋白酶抑制剂,Z-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor) 目录号 : GC15066An inhibitor of cysteine proteases, including cathepsin B
Cas No.:197855-65-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Z-FA-FMK is a control peptidic fluoromethylketone (boc-Thr-CH2F), and inhibitor to calpain (Ac-Leu-Leu-norleucinal), cathepsin B (Z-Phe-Ala-CH2F), and CPP32-like proteases (Z-DEVD-CH2F) [1]. A peptidyl fluoromethyl ketone (cathepsin B) was found to be an effective compound in a time dependent inactivation of cathepsin B isozymes from a number of tissues including human tumors [2]. The inhibitor of cathepsins B and L Z-FA-fmk blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective RRMs. Z-FA-FMK can inhibit caspase activity in vitro and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. In contrast, purified initiator caspases 8 and 10 are not affected, whereas the apoptosome-associated caspase 9 is only partially inhibited by Z-FA-FMK in vitro. [3]
It is an inhibitor of cysteine proteases, such as cathepsin B, which do not require a P1 Asp residue. It may be used as a negative control inhibitor for FMK P1 Asp caspase inhibitors.
References:
1. Inhibition of the interleukin-1 beta converting enzyme family rescues neurons from apoptotic death. Lynch, T., Vasilakos, J.P., Raser, K., Keane, K.M., Shivers, B.D. Mol. Psychiatry (1997)
2. Visualization of time-dependent inactivation of human tumor cathepsin B isozymes by a peptidyl fluoromethyl ketone using a fluorescent print technique. Smith, R.E., Rasnick, D., Burdick, C.O., Cho, K.J., Rose, J.C., Vahratian, A. Anticancer Res. (1988)
3. Lopez-Hernandez, F. J., Ortiz, M. A., Bayon, Y., & Piedrafita, F. J. (2003). 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 Pathway1. Molecular cancer therapeutics, 2(3), 255-263.
Cas No. | 197855-65-5 | SDF | |
别名 | 半胱氨酸蛋白酶抑制剂,Z-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor | ||
化学名 | benzyl N-[1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate | ||
Canonical SMILES | CC(C(=O)CF)NC(=O)C(CC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2 | ||
分子式 | C21H23N2O4F | 分子量 | 386.42 |
溶解度 | ≥ 13.45mg/mL in DMSO, ≥ 3.57 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5879 mL | 12.9393 mL | 25.8786 mL |
5 mM | 0.5176 mL | 2.5879 mL | 5.1757 mL |
10 mM | 0.2588 mL | 1.2939 mL | 2.5879 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。