MilliporeSigma™ Calbiochem™ MALT1 Inhibitor I, MI-2

Description

• A cell-permeable chloromethyl amide that inhibits MALT1 proteolytic activity (IC 50 = 5.84μM against MALT1 paracaspase domain dimer-catalyzed Ac-LRSR-AMC hydrolysis) in an irreversible manner via covalent interaction, displaying little or no activity against caspase-3, -8, or -9
• Due to irreversible binding and effective intracellular accumulation (HBL-1 intracellular [MI-2] t = 2 h = 5μM; Medium [MI-2] t = 0 = 0.2μM), MI-2 is at least 250-times more effective than Z-VRPR-FMK in blocking constitutive NF-κB activity and c-Rel nuclear translocation in HBL-1 cultures (equal or better blockage by 200nM MI-2 than by 50μM Z-VRPR-FMK)
• Shown to selectively inhibit MALT1-dependent ABC-DLBCL proliferation, but not the MALT1-independent growths of ABC- (HLY-1 and U2932) or GCB-DLBCL (OCI-Ly1 and OCI-Ly7) cells, both in cultures in vitro (GI 50 in 48 h = 200, 400, 400, and 500 nM, respectively, against HBL-1, OCI-Ly3, OCI-Ly10, and TMD8) and in mice in vivo (65%,, 61%, and 0% suppression, respectively, of HBL-1, TMD8, and OCI-Ly1 tumor expansion 24 h after 14 daily 25mg/kg/day i.p
• dosages) without any apparent toxicity to mice
• Please note that the molecular weight for this compound is batch-specific due to variable water content
• Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight
• The molecular weight provided represents the baseline molecular weight without water.