Ac-FLTD-CMK

  Cat. No.:  DC40142   Featured
Chemical Structure
2376255-48-8
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Field of application
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.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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