生物活性

Ac-YVAD-CMK is a cell-permeable and irreversible inhibitor of caspase-1 (K_i = 760 pM), caspase-4, and caspase-5. It also inhibits Fas-mediated apoptosis and acidic sphingomyelinase activation. Caspase inhibitors play an important role in investigating biological processes. The caspase family of proteins function as key components of the apoptotic machinery and act to destroy specific target proteins which are critical to cellular longevity. Caspase-1, originally designated ICE (for IL-1 converting enzyme), is a member of the group of caspases with large prodomains. Active caspase-1, a (p20/p10)₂ tetramer, is necessary and sufficient for cleavage of precursor IL-1 as well as for induction of apoptosis in some cell lines. Following use of the inhibitor, standard apoptosis assays can be used to examine treated cells for evidence of apoptosis.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Brenner, B., et al. 1998. Cell Death Differ. 5: 29-37. PMID: 10200443
[2] Garcia-Calvo, M., et al. 1998. J. Biol. Chem. 273: 32608-32613. PMID: 9829999
[3] Hilbi, H., et al. 1998. J. Biol. Chem. 273: 32895-32900. PMID: 9830039
[4] Thornberry, N.A., et al. 1998. Science. 281: 1312-1316. PMID: 9721091
[5] Schlegel, J., et al. 1996. J. Biol. Chem. 271: 1841-1844. PMID: 8567626

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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