MALT1 is a paracaspase, which is related to the caspase (cysteine-aspartic proteases) family of proteases but cleaves after Arg residues instead of Asp. MALT1 cleavage activity is linked to the pathogenesis of activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL), a chemoresistant form of DLBCL. MALT1 is a unique paracaspase protein that transduces aberrant oncogenic signaling in ABC-DLBCL. MALT1 represents a potentially important therapeutic target for ABC-DLBCL and MALT lymphoma. MALT1 small molecule inhibitors might be useful chemical tools for studying MALT1 biology and treating MALT1-addicted tumors.
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MI 2 MALT1 inhibitor
MI-2 (MALT1 inhibitor) is a selective, irreversible MALT1 paracaspase inhibitor with IC50 of 5.84 uM, displays little activity against the related caspase family members caspase-3, -8, and -9; inhibits cleavage of MALT1 substrates, which is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation; specifically suppress ABC-DLBCL in vitro and in vivo, exhibits GI 50 of 0.2, 0.5, 0.4, and 0.4 uM for HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells respectively, inhibits nuclear translocation of RelB and p50, and decreases Bcl-xL levels in CLL cells.
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