Uses
Ac-YVAD-CMK is a selective, irreversible inhibitor of interleukin-1β converting enzyme (ICE; Caspase-1). Ac-YVAD-CMK is neuroprotective in a rat model of cerebral ischemia.[Cayman Chemical]
Uses
Ac-YVAD-cmk has been used:
- as an inflammasome inhibitor to add to THP-1 cells or PBMC (peripheral blood mononuclear cell) before stimulation
- as a caspase-1 inhibitor injected to C57BL/6 mice
- as a caspase-1 inhibitor, administered into mice before and during hematopoietic stem cell transplantation (HSCT) to evaluate its effect on bone marrow inflammatory injury
- to abolish the histidine-rich protein II (HRPII) effect on transendothelial electrical resistance (TEER)
- as caspase 1 inhibitor, to treat MCF-7 tumor xenograft mice, to validate the role of inflammasomes activation in tumor growthin vivocondition
General Description
Interleukin-1β converting enzyme (ICE) is a cysteine protease that cleaves the IL-1β precursor to mature IL-1β. Caspase-1 inhibitor II is a cell-permeable, irreversible inhibitor of Caspase-1, Caspase-4, and Caspase-5. Inhibits CPP32/Apopain at a much higher concentration. Inhibits Fas-mediated apoptosis and acidic sphingomyelinase activation.
Biochem/physiol Actions
Ac-YVAD-cmk is a selective ireversible inhibitor of caspase-1 (interleukin-1β converting enzyme, ICE) with some activity also against caspase-4. Ac-YVAD-cmk is anti-apoptotic and has anti-inflammatory and neuroprotective effects, thought to result from its preventing caspase-1 activation of the proinflammatory cytokine, Interleukin-1β.
in vivo
Ac-YVAD-cmk treatment (1 μg/rats; SD rat; injected into the left lateral ventricle) significantly decreases the protein levels of caspase-1 (p20), mature IL-1β/IL-18 compared with the ICH group[2].
Ac-YVAD-cmk (rats with ac-YVAD-cmk at a dose of 12.5 μmol/kg) significantly reduces mortality from 83 to 33% using Log Rank analysis[3].
