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2376255-48-8

2376255-48-8 structure
2376255-48-8 structure
  • Name: Ac-FLTD-CMK
  • Chemical Name: Ac-FLTD-CMK
  • CAS Number: 2376255-48-8
  • Molecular Formula: C26H37ClN4O8
  • Molecular Weight: 569.05
  • Catalog: Signaling Pathways Apoptosis Caspase
  • Create Date: 2021-01-06 23:51:01
  • Modify Date: 2024-01-08 11:22:41
  • 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].

Name Ac-FLTD-CMK
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].
Related Catalog
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.

Molecular Formula C26H37ClN4O8
Molecular Weight 569.05
Hazard Codes Xi