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.
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KEA1-97 (KEA 1-97) is a small molecule that disrupts the interaction of thioredoxin with caspase 3; activates caspases, and induces apoptosis without affecting thioredoxin activity, impairs triple-negative breast cancer cell survival; impairs in vivo breast tumor xenograft growth.
MLT-748 (MLT748) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 5 nM, does not show inhibitory activity against 22 other tested human proteases (IC50>100 uM); binds MALT1 in the allosteric Trp580 pocket, reversibly binds and stabilizes human mutant MALT1-W580S with Kd of 13 nM, with affinity similar to that of the wild type MALT1 (Kd=42 nM); stabilizes MALT1-W580S in MALT1mut/mut B cells with EC50 of 69 nM, blocks cleavage of MALT1 substrates in human lymphocytes, including HOIL1, RelB, CYLD, and BCL10 (BCL10 cleavage IC50=31 nM), rescues MALT1 function in patient MALT1mut/mut lymphocytes.
MLT-747 (MLT747) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 14 nM; binds MALT1 in the allosteric Trp580 pocket, reversibly binds and stabilizes human mutant MALT1-W580S in vitro and in MALT1mut/mut B cells, inhibits MALT1 peptide cleavage.
MALT1 paracaspase inhibitor 3
MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk; binds covalently to the catalytic cysteine (C464) of MALT1, induces MALT1 oligomerization; exhibits potent activity in the Raji-GloSensor MALT1 protease inhibition (IC50=60 nM) and OCI-Ly3 growth inhibition assays (IC50=0.1 uM), selectively inhibits the growth of MALT1 dependent cell lines by decreasing cell proliferation and increasing apoptosis; downregulated IL10 protein expression in vitro and in vivo, also decreases STAT3 phosphorylation in ABC DLBCL cells; suppresses the growth of ABC DLBCL tumors in vivo.
VX-765 (Belnacasan) is an orally absorbed prodrug of VRT-043198, which is a potent and selective inhibitor of interleukin-converting enzyme/caspase-1 with Ki of 0.8 nM; VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9, VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases; inhibits LPS-induced IL-1β production, reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.
BOC-D-FMK is a cell-permeable, irreversible, broad spectrum caspase inhibitor, inhibits apoptosis stimulated by TNF-α with IC50 of 39 uM; inhibits TNFα-stimulated reactive oxygen species (ROS) generation, prevents genistein-induced apoptosis of p815 cells at 50 uM; shows neuroprotective effects on spinal motoneurons (MNs) after root avulsion in neonatal rats, suppresses polyethylene particle-induced osteolysis in mice.
Q-VD-Oph is a potent pan-caspase inhibitor, inhibits human recombinant caspase-7 with IC50 of 48 nM in cell-free assay, also inhibits caspase -1, 3, 8, 9, 10, and 12 with IC50 of 25-400 nM; reduces doxorubicin-induced caspase-3 activation, increases expression of p21/WAF1 and senescence -associated -beta-galactosidase activity, but does not alter Akt activation, Q-VD-Oph is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk; prevents activated caspase-7 and caspase-cleaved fragments of tau in the TgCRND8 brain, as well as pathology associated with TgCRND8 mice.
Z-DEVD-FMK is a specific caspase-3 inhibitor with IC50 of 18 uM; affects the survival and function of platelets in platelet concentrate during storage, blocks the geranylgeraniol-induced DNA fragmentation in human leukemia cells; abolishes the apoptosis, CPP32/Mch3alpha processing and the increase in CPP32-like protease activity induced by TGF-beta1 in rat hepatocytes.
Emricasan (IDN-6556;PF-03491390) is a potent, irreversible pan-caspase inhibitor, shows neuroprotective activity for hNPCs, inhibits ZIKV-induced increased caspase-3 activity.
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