MALT1-MI-2 (MI-2), MALT1 inhibitor


Catalog No. size PriceQuantity
M60098-2D 10 mM DMSO (0.439 mL) $129
M60098-2S 2mg solid $129
M60098-25S 25mg solid $550

Description

Product Information
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.

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