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Ac-YVAD-cmk

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Chemical Structure| 178603-78-6 同义名 : Caspase-1 Inhibitor II;​N-Ac-Tyr-Val-Ala-Asp-CMK;N-Ac-Tyr-Val-Ala-Asp-CMK
CAS号 : 178603-78-6
货号 : A1329237
分子式 : C24H33ClN4O8
纯度 : 99%+
分子量 : 540.994
MDL号 : MFCD00237124
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(194.09 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Caspase-1 is a key enzyme of the NLRP3 inflammasome, which is a critical pro-inflammatory mediator that modulates host responses to various stress conditions[3]. Ac-YVAD-CMK inhibited activation of M1 microglial and enhanced M2 microglial activation after ICH (Intracerebral hemorrhage)[4]. In mice, Caspase-1 activation was inhibited significantly in a dose-dependent manner by pretreatment with AC-YVAD-CMK (1.25, 6.25, and 12.5 μmol/kg). Furthermore, AC-YVAD-CMK (12.5 μmol/kg) pretreatment significantly reduced the cold-restraint stress induced multiple haemorrhagic gastric erosions and ulcers, as well as the elevated levels of IL-1β, IL-18 and CD68 mRNA expression. Treatment of mice with AC-YVAD-CMK (12.5 μmol/kg) 30 min before cold-stress injury decreased the mortality rate compared with mice that received vehicle. Moreover, AC-YVAD-CMK (12.5 μmol/kg) alleviated the overexpression of phospho (P)-P38 protein and P-IκB induced by cold-restraint stress. In addition, ethanol induced multiple haemorrhagic erosions and ulcers were also alleviated significantly by pretreatment with AC-YVAD-CMK (12.5 μmol/kg)[3]. AC-YVAD-CMK treatment improved rotarod performance time after 72 hrs as compared with ICH group[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.24mL

1.85mL

0.92mL

18.48mL

3.70mL

1.85mL

参考文献

[1]Kondo S, Barna BP, Morimura T, Takeuchi J, Yuan J, Akbasak A, Barnett GH. Interleukin-1 beta-converting enzyme mediates cisplatin-induced apoptosis in malignant glioma cells. Cancer Res. 1995 Dec 15;55(24):6166-71. PMID: 8521409.

[2]Kondo S, Kondo Y, Yin D, Barnett GH, Kaakaji R, Peterson JW, Morimura T, Kubo H, Takeuchi J, Barna BP. Involvement of interleukin-1 beta-converting enzyme in apoptosis of bFGF-deprived murine aortic endothelial cells. FASEB J. 1996 Aug;10(10):1192-7. doi: 10.1096/fasebj.10.10.8751721. PMID: 8751721.

[3]Zhang F, et al. The caspase-1 inhibitor AC-YVAD-CMK attenuates acute gastric injury in mice: involvement of silencing NLRP3 inflammasome activities. Sci Rep. 2016 Apr 7;6:24166

[4]Lin X, et al. AC-YVAD-CMK Inhibits Pyroptosis and Improves Functional Outcome after Intracerebral Hemorrhage. Biomed Res Int. 2018 Oct 16;2018:3706047