Caspase 4 Inhibitor

Ac-DEVD-CHO is a Caspase-3 inhibitor with a K_i value of 230 pM.

VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits K_i values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.

Z-LEVD-FMK is a cell-permeable caspase-4 inhibitor. Z-LEVD-FMK blocks ER stress-induced apoptosis in cancer cells.

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.

Caspase-4-IN-1 (compound 35) is a selective allosteric caspase-4 inhibitor that spares caspase-1, and in embodiments acts as a dual caspase-4/5 inhibitor.

Ac-LEVD-CHO is a caspase-4 inhibitor. Ac-LEVD-CHO is a peptide with the sequence of Ac-Leu-Glu-Val-Asp-al.

ML132 (NCGC-00183434) is a selective caspase 1 inhibitor with an IC₅₀ value of 0.023 nM. ML132 has good stability and can be used as a caspase 1 molecular probe. ML132 is applicable to research in the fields of anticancer and anti-inflammatory studies.

Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC₅₀s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.

Z-LEED-FMK is a caspase-13 and caspase-4 inhibitor. Z-LEED-FMK also inhibits caspase-1 processing in S. typhimurium-infected macrophages.

Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity.