For research use only. Not for therapeutic Use.
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].
SET2 (20 μM; 24 h) abrogates the migration of PC-3M cells expressing TRPV2[1].
SET2 (20 μM; 24 h) inhibits 2-APB-evoked current in HEK293T cells transiently co-transfected with TRPV2 and LPAR1[1].
SET2 (20 μM; 24 h) inhibits the increase of (0.1 μM; 3 min) LPA-induced cytoplasmic calcium and LPA-induced migration in PC-3M cells[1].
| Catalog Number | I041804 |
| CAS Number | 2313525-20-9 |
| Synonyms | N-(furan-2-ylmethyl)-3-[4-[methyl(propyl)amino]-6-(trifluoromethyl)pyrimidin-2-yl]sulfanylpropanamide |
| Molecular Formula | C17H21F3N4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C17H21F3N4O2S/c1-3-7-24(2)14-10-13(17(18,19)20)22-16(23-14)27-9-6-15(25)21-11-12-5-4-8-26-12/h4-5,8,10H,3,6-7,9,11H2,1-2H3,(H,21,25) |
| InChIKey | LZHSWRWIMQRTOP-UHFFFAOYSA-N |
| SMILES | CCCN(C)C1=NC(=NC(=C1)C(F)(F)F)SCCC(=O)NCC2=CC=CO2 |
| Reference | [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. |
