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Z-FA-FMK

 
Catalog No.
A8170
半胱氨酸蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,272.00
现货
1mg
¥ 545.00
现货
5mg
¥ 1,818.00
现货
10mg
¥ 3,272.00
现货
25mg
¥ 3,636.00
现货

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A

背景

Z-FA-FMK是一种对照多肽氟甲基酮(boc-Thr-CH2F),是钙蛋白酶(Ac-Leu-Leu-norleucinal)、组织蛋白酶B(Z-Phe-Ala-CH2F)以及CPP32样蛋白酶(Z-Phe-Ala-CH2F)的抑制剂 [1]。在包括人类肿瘤的多种组织中,多肽氟甲基酮是引起组织蛋白酶B同工酶失活的有效化合物,以时间依赖性的方式发挥作用[2]。组织蛋白酶B和L的抑制剂Z-FA-FMK阻断选择性RRMs诱导的DEVDase活性、DNA片段化和磷脂酰丝氨酸外化。Z-FA-FMK可以抑制体外caspase活性,选择性的抑制重组效应子caspases-2、-3、-6和-7。相比之下,纯化的起始caspases 8和10不受影响,而凋亡体相关的caspase 9仅部分被抑制[3]。

Z-FA-FMK是半胱氨酸蛋白酶的抑制剂,如组织蛋白酶B,不需要P1 Asp残基。它可被用作FMK P1 Asp caspase抑制剂的阴性对照抑制剂。

参考文献:
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.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt386.42
Cas No.105637-38-5;197855-65-5
FormulaC21H23N2O4F
SynonymsZ-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor
Solubilityinsoluble in H2O; ≥13.45 mg/mL in DMSO; ≥3.57 mg/mL in EtOH with ultrasonic
Chemical Namebenzyl N-[1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate
SDFDownload SDF
Canonical SMILESCC(C(=O)CF)NC(=O)C(CC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

Cell experiment:[1]

Cell lines

Jurkat T cells

Reaction Conditions

5, 30, or 100 μM Z-FA-FMK for 1 h preincubation

Applications

Increasing concentrations of Z-FA-FMK prevented retinoid-related molecule (RRM)-induced DNA fragmentation and DEVDase activity. Similarly, preincubation with a high concentration of Z-FA-FMK (100 μM) significantly inhibited the externalization of phosphatidylserine induced by RRMs. Z-FA-FMK, as an inhibitor of cathepsins B and L, has been used to explore the molecular mechanism underlying the anticancer activity of RRMs.

Animal experiment:[2]

Animal models

SCID mice xenografted with Ras oncogenic HT1080 cells

Dosage form

0.02 mg

Administered intratumorally, everyday up to 7 days post-viral injection and every 2 days until completion of the experiment.

Applications

Z-FA-FMK effectively blocked the replication activity of respiratory enteric orphan (reo)virus in both tumor and hear tissues. Therefore, Z-FA-FMK could serve as a potential viral inhibitor which prevents reovirus-mediated myocarditis and oncolysis in vivo.

Note

The technical data provided above is for reference only.

References:

1. Lopez-Hernandez FJ, Ortiz MA, Bayon Y, 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. Molecular Cancer Therapeutics, 2003, 2(3): 255-263.

2. Kim M, Hansen KK, Davis L, et al. Z-FA-FMK as a novel potent inhibitor of reovirus pathogenesis and oncolysis in vivo. Antiviral Therapy, 2010, 15(6): 897-905.

生物活性

Description Z-FA-FMK是半胱氨酸蛋白酶的不可逆抑制剂
靶点 cysteine protease          
IC50            

质量控制

化学结构

Z-FA-FMK

相关生物数据

Z-FA-FMK

相关生物数据

Z-FA-FMK