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Ac-FLTD-CMK
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。
Ac-FLTD-CMK图片
CAS NO:2376255-48-8
包装:1mg
市场价:3330元

产品介绍
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。
Cas No.2376255-48-8
Canonical SMILESClCC([C@H](CC(O)=O)NC([C@H]([C@H](O)C)NC([C@H](CC(C)C)NC([C@@H](NC(C)=O)CC1=CC=CC=C1)=O)=O)=O)=O
分子式C26H37ClN4O8
分子量569.05
储存条件Store at -20°C, protect from light, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.