Ac-FLTD-CMK是胃泌素D(GSDMD)衍生的抑制剂，是炎症性caspases的特异性抑制剂。Ac-FLTD-CMK对caspases-1(IC50为46.7nM)，caspases-4(IC50为1.49μM)，caspases-5(IC50为329nM)和caspases-11均有效，但对凋亡相关的caspase-3无效。
货号:ajcx30112
CAS:2376255-48-8
分子式:C26H37ClN4O8
分子量：569.05
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is potent against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3[1].

Ac-FLTD-CMK, inhibits GSDMD cleavage by caspases-1, -4, -5, and -11 in vitro, suppresses pyroptosis downstream of both canonical and noncanonical inflammasomes, as well as reduces IL-1β release following activation of the NLRP3 inflammasome in macrophages. By contrast, Ac-FLTD-CMK does not target caspase-3 or apoptotic cell death. Crystal structure of caspase-1 in complex with Ac-FLTD-CMK reveals extensive enzyme-inhibitor interactions involving both hydrogen bonds and hydrophobic contacts[1].

[1]. Jie Yang, et al. Mechanism of gasdermin D recognition by inflammatory caspases and their inhibition by a gasdermin D-derived peptide inhibitor. Proc Natl Acad Sci U S A. 2018 Jun 26;115(26):6792-6797.