|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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.
How to Use:
- In vitro: MALT1-MI-2 (MI-2) was used at 0.2-2 µM concentration in vitro and cellular assays.
- In vivo: MALT1-MI-2 (MI-2) was intraperitoneally (IP) dosed to mice at 25 mg/kg once per day for 14 days in TMD8 and HBL-1 ABC-DLBCL xenografts.
- 1. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. (2012) Cancer Cell. 22(6):812-24.
Products are for research use only. Not for human use.
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