MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to mice[1]. IC50: 5.84 μM (MALT1)[1]
MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 µM, respectively[1].MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[1]. Cell Proliferation Assay[1] Cell Line: HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells
MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts[1]. Animal Model: Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1]
[1]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.