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.

References 1. Fontán L, et al. J Clin Invest. 2018 Jul 19. pii: 99436. View Related Products by Target Caspase