SET2

SET2 is an inhibitor of transient receptor potential vanilloid 2 (TRPV2, IC50 = 0.46 µM). It selectively inhibits currents induced by the TRP channel modulator 2-APB (Cay-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 (Cay-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.Formal Name: N-(2-furanylmethyl)-3-[[4-(methylpropylamino)-6-(trifluoromethyl)-2-pyrimidinyl]thio]-propanamide. CAS Number: 2313525-20-9. Molecular Formula: C17H21F3N4O2S. Formula Weight: 402.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Sparingly soluble: 1-10 mg/ml. SMILES: O=C(CCSC1=NC(C(F)(F)F)=CC(N(CCC)C)=N1)NCC2=CC=CO2. InChi Code: 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). InChi Key: LZHSWRWIMQRTOP-UHFFFAOYSA-N.