Signaling Pathway

Caspase

Caspase

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Caspase is a family of cysteine proteases that play essential roles in apoptosis (programmed cell death), necrosis, and inflammation. There are two types of apoptotic caspases: initiator (apical) caspases and effector (executioner) caspases. Initiator caspases (e.g., CASP2, CASP8, CASP9, and CASP10) cleave inactive pro-forms of effector caspases, thereby activating them. Effector caspases (e.g., CASP3, CASP6, CASP7) in turn cleave other protein substrates within the cell, to trigger the apoptotic process. The initiation of this cascade reaction is regulated by caspase inhibitors. CASP4 and CASP5, which are overexpressed in some cases of vitiligo and associated autoimmune diseases caused by NALP1 variants, are not currently classified as initiator or effector in MeSH, because they are inflammatory enzymes that, in concert with CASP1, are involved in T-cell maturation.

Caspase Inhibitors & Modulators (11)

Product Name Catalog No. Brief Description
ASK1-IN-1

HY-100844

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor extracted from patent WO2016025474A1, Compound 4.

BOC-D-FMK

HY-13229

BOC-D-FMK is a pan-caspase inhibitor.

Laquinimod

HY-13010

Laquinimod (ABR-215062) is a potent immunomodulator.

NQDI-1

HY-19566

NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM.

PAC-1

HY-13523

PAC-1(Procaspase-activating compound-1) is the first direct caspase-activating compound with EC50 of 0.22 uM; enhances the activity of procaspase-3 in vitro and induces apoptotic death in cancer cells in culture and in mouse xenograft models.

Q-VD-OPh

HY-12305

Q-VD-OPha is a pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 1, 3, 8 and 9 with IC50 values of 50, 25, 100, and 430 nM, respectively.

Selonsertib

HY-18938

GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain.

Silvestrol

HY-13251

Silvestrol, a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7; 5'myc-UTR-LUC inhibtior (IC50= 0.8 nM).

VX-765

HY-13205

VX-765(Belnacasan) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM.

Z-DEVD-FMK

HY-12466

Z-DEVD-FMK(Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

Z-VAD-FMK

HY-16658

Z-VAD-FMK is a cell-permeable, irreversible broad-spectrum caspase inhibitor, blocks all features of apoptosis.