Description
SET2 is a novel selective TRPV2 antagonist.
Uses
SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases[1].
IC 50
TRPV2: 0.46 μM (IC
50)
References
[1] Chai H, et al. Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. J Med Chem. 2019 Feb 14;62(3):1373-1384. DOI:
10.1021/acs.jmedchem.8b01496