Cas No.: | 2376255-48-8 |
Chemical Name: | CID 155906572 |
Synonyms: | CID 155906572;Ac-FLTD-CMK |
SMILES: | ClC([H])([H])C([C@]([H])(C([H])([H])C(=O)O[H])N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O)=O)=O)=O |
Formula: | C26H37ClN4O8 |
M.Wt: | 569.0470 |
Purity: | >98% |
Sotrage: | -20°C, protect from light, stored under nitrogen*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
Description: | Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective 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]. |
Target: | Caspase-1:46.7 nM (IC50) Caspase-4:1.49 μM (IC50) Caspase-5:329 nM (IC50) Caspase-11 |
In Vitro: | 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]. |
References: | [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. |