| Molecular Weight: | 455.72 |
| Formula: | C19H17Cl3N4O3 |
| Purity: | ≥ 98% |
| CAS#: | 1047953-91-2 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 2-chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
Reference:
- 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.
