BVT 948, 10 mg

BVT 948 is a non-competitive, cell-permeable and irreversible inhibitor of protein tyrosine phosphatases (IC50 are 0.9 µM, 1.7 µM, 0.09 µM, 1.5 µM and 0.7 µM for PTP1B, TCPTP, SHP-2, LAR, YopH). It displays irreversible inhibition through catalyzing the hydrogen peroxide dependent oxidation of the enzyme, and led to the specific oxidation of the catalytic cysteine.  In cell-based assays, BVT 948 increased the tyrosine phosphorylation level of the insulin receptor and thus enhances insulin signaling. BVT 948 was also efficiently inhibiting several cytochrome P450 isoforms in vitro (IC50 < 10 μM).

Solubility: ethanol/DMSO to 50 mM, Molecular Weight:  241.3 g/mol, CAS Number: 39674-97-0

Formula: C₁₄H₁₁N₃

Product specific literature references:

Liljebris C, Baranczewski P, Björkstrand E, Bystr�m S, Lundgren B, Tjernberg A, Warol�n M, James SR. (2004) "Oxidation of protein tyrosine phosphatases as a pharmaceutical mechanism of action: a study using 4-hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione." J Pharmacol Exp Ther. 309(2):711-9.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.