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Beschreibung

A cell-permeable phenothiazine that that inhibits MALT1, but not caspase-3 or -8, proteolytic activity (IC50 = 0.83 and 0.42 µ,M, respectively, against full-length or paracaspase domain-catalyzed Ac-LRSR-AMC hydrolysis) in a reversible and noncompetitive manner. Shown to suppress ABC-DLBCL constitutive cellular MALT1 activity (by >75% at 10 µ,M, IC50<5 µ,M in U2932, OCI-Ly10, OCI-Ly3, HBL1, and TMD8 cultures) and RelB cleavage, resulting in ABC-DLBCL-selective cytotoxicity (>=27% cell death in 4 days at 10 µ,M) over GCB-DLBCL (<=26% cell death in 4 days at 20 µ,M) both in cultures in vitro and in mice (400 µ,g/kg daily i.p.) in vivo.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., MALT1 Inhibitor II, Mepazine HCl, CAS 60-89-9, is a cell-permeable inhibitor of MALT1. Does not affect caspase-3 or -8 activities., A cell-permeable phenothiazine that inhibits MALT1, but not caspase-3 or -8, proteolytic activity (IC50 = 0.83 and 0.42 µ,M, respectively, against full-length or paracaspase domain-containing aa 325-760 MALT1 GST fusion-catalyzed Ac-LRSR-AMC hydrolysis) in a reversible and noncompetitive manner and blocks anti-CD3/CD28-stimulated IL-6 production (20 h) in primary murine CD4+ T-cell (by 77%) and human PBMC cultures (by 51 - 89%). Shown to suppress ABC-DLBCL constitutive cellular MALT1 activity (>75% suppression by 10 µ,M Mepazine, IC50<5 µ,M in U2932, OCI-Ly10, OCI-Ly3, HBL1, and TMD8 cultures) and RelB cleavage, resulting in effective blockage of NF-kappaB-dependent IL-6, IL-10, as well as anti-apoptotic Bcl-xL and FLIP-L expressions. Mepazine exhibits ABC-DLBCL-selective cytotoxicity (>=27% cell death in 4 days by 10 µ,M Mepazine in HBL-1, OCI-Ly3, OCI-Ly10, TMD8, and U2932 cultures) over GCB-DLBCL (<=26% cell death in 4 days by 20 µ,M Mepazine in DJAB, Su-DHL-4, and Su-DHL-6 cultures) both in cultures in vitro and in mice (74%, and 0% suppression, respectively, of OCI-Ly10 and Su-DHL-6 tumor expansion on day 22 post cancer transplant, via daily 400 µ,g/kg i.p.) in vivo.