SIRT1/2 Inhibitor IV

SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner. It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases. By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest. It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1alpha protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.Formal Name: 2,3-dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone. CAS Number: 14513-15-6. Synonyms: Cambinol, NSC 112546, SIRT1 Inhibitor II, SIRT2 Inhibitor VI. Molecular Formula: C21H16N2O2S. Formula Weight: 360.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml, Ethanol: 0.33 mg/ml. lambdamax: 228, 281 nm. SMILES: S=C1NC(C(CC2=C(C=CC=C3)C3=CC=C2O)=C(C4=CC=CC=C4)N1)=O. InChi Code: InChI=1S/C21H16N2O2S/c24-18-11-10-13-6-4-5-9-15(13)16(18)12-17-19(14-7-2-1-3-8-14)22-21(26)23-20(17)25/h1-11,24H,12H2,(H2,22,23,25,26). InChi Key: RVNSQVIUFZVNAU-UHFFFAOYSA-N.