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MX1013
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。
MX1013图片
规格:98%
分子量:382.4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
MX1013 是一种有效的、不可逆的二肽半胱天冬酶抑制剂,具有抗细胞凋亡活性。 MX1013 抑制重组人 caspase 3,IC50 为 30 nM。
货号:ajcx19530
CAS:582316-00-5
分子式:C18H23FN2O6
分子量:382.4
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 10 mg/ml
纯度:98%
存储:Store at -20°C
库存:现货

Background:

MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1 (IC50 = 20 nM), caspase-3 (IC50 = 30 nM), and caspase-6, -7, -8, and -9 (IC50s = 5-18 nM).1 It is selective for caspases over calpain I, cathepsin B, cathepsin D, renin, thrombin, and Factor Xa (IC50s = >10 μM). MX1013 (0.05 μM) inhibits anti-Fas antibody-induced caspase-3 processing and poly(ADP)ribose polymerase (PARP) cleavage in Jurkat cells, indicating inhibition of apoptosis. It increases survival in a mouse model of anti-Fas antibody-induced liver failure when administered at doses of greater than or equal to 0.25 mg/kg. MX1013 reduces infarct size in rat models of acute myocardial infarction-reperfusion or transient focal brain ischemia-reperfusion injury when administered intravenously as a 20 mg/kg bolus dose followed by a 5 mg/kg per hour infusion.

参考文献
1. Yang, W., Guastella, J., Huang, J.-C., et al. MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity. Br. J. Pharmacol. 140(2), 402-412 (2003).