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SET2 is an inhibitor of transient receptor potential vanilloid 2 (TRPV2; IC50 = 0.46 µM).1 It selectively inhibits currents induced by the TRP channel modulator 2-APB (Item No. 64970) in a patch-clamp assay using HEK293T cells overexpressing TRPV2 at 0.3 or 1 µM over HEK293T cells overexpressing TRPV1 or TRPV3 at 3 or 10 µM. SET2 (20 µM) reduces migration induced by lysophosphatidic acid (LPA) in PC-3M prostate cancer cells to a similar extent as the LPA receptor 1 (LPA1) antagonist AM966 (Item No. 22048). It also reduces LPA-induced increases in current in a patch-clamp assay using HEK293T cells when used at a concentration of 10 µM.
WARNING This product is not for human or veterinary use.
1. Structure-