Drug intelligence / Profile preview

Ac-YVAD-CHO

Development stage
Preclinical
Lead developer
Merck KGaA
Modality
Peptides, Small Molecules
Administration
Inhalation, Intranasal, Intraperitoneal, Intravenous
01

Overview

Ac-YVAD-CHO (also known as L-709049) is a potent, selective, and reversible peptide-based inhibitor of caspase-1 (interleukin-1β converting enzyme, ICE) with a Ki of approximately 0.76 nM. It is highly selective for caspase-1 over other caspases, such as caspase-2, -3, -4, -5, -6, -7, -8, -9, and -10. Ac-YVAD-CHO acts by binding to the active site of caspase-1, preventing the proteolytic cleavage of pro-interleukin-1β (pro-IL-1β) and pro-interleukin-18 (pro-IL-18) into their mature, active inflammatory forms, thereby suppressing pyroptosis and inflammatory responses. While primarily utilized as a research-use-only reagent to study inflammasome activation, apoptosis, and pyroptosis, it has also been investigated in preclinical models of inflammatory diseases, acute pancreatitis, endotoxemia, and breast cancer.

Other names
Ac-Tyr-Val-Ala-Asp-CHOCaspase-1 Inhibitor ICaspase1 Inhibitor ICaspase 1 Inhibitor IICE Inhibitor IN-Ac-Tyr-Val-Ala-Asp-CHON-acetyl-L-tyrosyl-L-valyl-N-[(1S)-2-carboxyl-1-formylethyl]-L-alaninamideYVAD-CHO
02

Targets

CASP4 (Caspase-4)CASP1 (Caspase-1)CASP5 (Caspase-5)

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