RK-682 is a protein tyrosine phosphatase inhibitor (IC50s = 54 µM for CD45, 2.0 µM for VHR, did not inhibit cdc25B) originally isolated from the fermentation of Streptomyces sp. 88-682.1 Inhibits cell cycle at G1/S. RK-682 has also been shown to inhibit PLA2 (IC50 = 16 µM)2, HIV-1 protease (IC50 = 84 µM)3, and heparanase (IC50 = 17 µM)4. Natural RK-682 (R-isomer) and synthetic racemic material have identical phosphatase activity.5 Care should be taken when using RK-682 in the presence of metal salts - RK-682 readily forms metal complexes that affects its phosphatase inhibitory activity.6 RK-682 has been identified as a potential promiscuous inhibitor.7
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