Z-FA-FMK

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Z-FA-FMK

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

197855-65-5

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
50mg	电议

产品名称

(1S)-Z-FA-FMK

产品介绍

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 potentCathepsin Band Linhibitor. 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 inhibitsapoptosis. Z-FA-FMK inhibitscaspaseactivity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is aviralinhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host^[1]^[2]^[3].

IC₅₀& Target^[1]

Cathepsin B

cathepsin L

Caspase-2

Caspase-3

Caspase-6

Caspase-7

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^[1].
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^[1].
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^[1].
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^[2].
Z-FA-FMK (20 μM; 48 h; HT1080 cells) induces defects in reoviral maturation^[2].

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^[2].
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^[3].

Animal Model:	SCID mice with HT1080 xenograft (6-8 weeks)^[2]
Dosage:	1 mg/kg
Administration:	Intratumor injection; every 2 days, for 27 days
Result:	Blocked reovirus replication activity in both tumor and heart tissues.

Animal Model:	Male BALB/c mice^[3]
Dosage:	8 mg/kg
Administration:	Intravenous injection; once, 1 hour later, intraperitoneal injection D-GalN (700 mg/kg) and TNF-α (15 μg/kg).
Result:	Decreased in the D-GalN/TNF-α-induced degenerative changes. Decreased in the number of activated caspase-3-positive tubular epithelial cell. Increased in kidney GSH levels, CAT, SOD and GPx activities and decreased in kidney LPO levels, LDH activity, serum AST and ALT activities, uric acid, and urea levels were determined.

分子量

386.42

性状

Solid

Formula

C₂₁H₂₃FN₂O₄

CAS 号

197855-65-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL(646.96 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

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

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
2.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.
请依序添加每种溶剂： 10% DMSO 90%corn oil
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。