MALT1-MI-2 (MI-2) --- MALT1 inhibitor
Overview | |
Catalog # | bs-60098c-2mg-solid |
Product Name | MALT1-MI-2 (MI-2) --- MALT1 inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 455.72 Formula: C19 H17 Cl3 N4 O3 CAS Number: 1047953-91-2 InChi Key: TWJGQZBSEMDPQP-UHFFFAOYSA-N InChi: InChI=1S/C19H17Cl3N4O3/c1-28-8-9-29-19-24-18(12-2-7-15(21)16(22)10-12)26(25-19)14-5-3-13(4-6-14)23-17(27)11-20/h2-7,10H,8-9,11H2,1H3,(H,23,27) Smiles: COCCOC1N=C(C2=CC(Cl)=C(Cl)C=C2)N(N=1)C1C=CC(=CC=1)NC(=O)CCl Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | MALT1-MI-2 (MI-2) is a highly potent and selective small molecule directly binding to MALT1 and irreversibly suppressing its protease function. MI-2 concentrated within human ABC-DLBCL cells and irreversibly inhibited cleavage of MALT1 substrates with EC50 < 1 µM (HBL-1 ~200 nM; TMD8 ~500 nM). This was accompanied by NF-κB pathway suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MI-2 was nontoxic to mice, and displayed selective activity against ABC-DLBCL cell lines in vitro and xenotransplanted ABC-DLBCL tumors in vivo. It was also effective against primary human non-germinal center B cell-like DLBCLs ex vivo. |