Z-FA-FMK (Synonyms: (1S)-Z-FA-FMK)
目录号: PL05759 纯度: ≥98%
CAS No. :197855-65-5
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中文名称
Z-FA-FMK
中文别名
NALPHA-[(苄氧基)羰基]-N-(4-氟-3-氧代-2-丁烷基)苯丙氨酰胺
英文名称
Z-FA-FMK
英文别名
Carbamic acid,N-[(1S)-2-[(3-fluoro-1-methyl-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-,phenylmethyl ester;Z-PHE-DL-ALA-FLUOROMETHYLKETONE;Carbamic acid,N-[(1S)-2-[(3-fluoro-1-methyl-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-,p...;Z-FA-FMK;Nalpha-[(Benzyloxy)Carbonyl]-N-(4-Fluoro-3-Oxo-2-Butanyl)Phenylalaninamide;Nalpha-[(Benzyloxy)Carbonyl]-N-(4-Fluoro-3-Oxo-2-Butanyl)Phenylalaninamide z-fa-fmk;benzyl N-[(2R)-1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate;Zfa-fmk;benzyl N-[(1S)-1-[(4-fluoro-3-oxobutan-2-yl)carbamoyl]-2-phenylethyl]carbamate;Carbamic acid, N-[(1S)-2-[(3-fluoro-1-methyl-2-oxopropyl)amino]-2-oxo-1-(phenylmethyl)ethyl]-, phenylmethyl ester;C21H23FN2O4;benzyl N-[(2S)-1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate;Carbamic acid, N-((1S)-2-((3-fluoro-1-methyl-2-oxopropyl)amino)-2-oxo-1-(phenylmethyl)ethyl)-, phenylmethyl este;(DL-alanine)-mdl-201053;Benzyl ((2S)-1-((4-fluoro-3-oxobutan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate;MDL-201053, (DL-ALANINE)-;N-Benzyloxycarbonyl-N-(3-fluoro-1-methyl-2-oxopropyl)-2-amino-3-phenyl-(2S)-propanamide
Cas No.
197855-65-5
分子式
C21H23FN2O4
分子量
386.42
包装储存
-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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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