PDD00017273

PDD00017273 is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor (IC50 = 26 nM in an enzyme assay). It maintains persistence of nuclear PAR chains in HeLa cells induced by the DNA damaging agent methylmethanesulfonate (MMS, IC50 = 37 nM). PDD00017273, in combination with MMS, increases nuclear phosphorylated H2AX (gammaH2AX) intensity, a marker of DNA double strand breaks, in MCF-7 cells in a concentration-dependent manner. It reduces clonogenic growth of ZR-75-1 and MDA-MB-436 cells but not HCC1937 cells (IC50s = 0.2, 0.8, and >10 µM, respectively).Formal Name: 1-[(1,3-dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide. CAS Number: 1945950-21-9. Molecular Formula: C23H26N6O4S2. Formula Weight: 514.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 10 mg/ml. lambdamax: 227 nm. SMILES: O=S(C1=CC=C(N(CC2=CC(C)=NN2C)C(N3CC4=CN=C(C)S4)=O)C(C3=O)=C1)(NC5(CC5)C)=O. InChi Code: InChI=1S/C23H26N6O4S2/c1-14-9-16(27(4)25-14)12-28-20-6-5-18(35(32,33)26-23(3)7-8-23)10-19(20)21(30)29(22(28)31)13-17-11-24-15(2)34-17/h5-6,9-11,26H,7-8,12-13H2,1-4H3. InChi Key: IFWUBRBMMNTBRZ-UHFFFAOYSA-N.