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.
Product information
CAS Number: 1047953-91-2
Molecular Weight: 455.72
Formula: C19H17Cl3N4O3
Chemical Name: 2-chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide
Smiles: COCCOC1N=C(C2=CC(Cl)=C(Cl)C=C2)N(N=1)C1C=CC(=CC=1)NC(=O)CCl
InChiKey: 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)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
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.
References:
- 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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