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Cat. No. Product Name CAS No. Information
PC-60171

KEA1-97

2138882-71-8

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.

PC-36043

MLT-747

2097853-86-4 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.
PC-36042

MLT-748

1832578-30-9 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.
PC-35426

MALT1 paracaspase inhibitor 3

2088355-90-0 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.
PC-63279

ML132

1230628-71-3 ML132 (NCGC-00183434, CID-4462093) is a highly potent, selective Caspase 1 inhibitor with IC50 of 0.023 nM, displays >1,000-fold selectivity over a panel of 9 caspases.
PC-43410

BOC-D-FMK

634911-80-1 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.
PC-43391

VX-765

273404-37-8 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.

Epilepsy

Phase 2 Discontinued

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