PCNA-I1

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells. It preferentially inhibits growth of a variety of human and mouse cancer cell lines (IC50s = 0.05-0.3 µM) over non-transformed cells (IC50s = 0.99-2 µM). PCNA-I1 leads to an accumulation of cells in the G1 phase during the first 24 hours of incubation and halts the cell cycle in the S and G2/M phases by 72 hours following treatment. It also reduces tumor growth in an LNCaP prostate cancer mouse xenograft model when administered at a dose of 10 mg/kg, five days per week, for two weeks.Formal Name: 3-methyl-2-[(1-hydroxy-2-naphthalenyl)methylene]hydrazide-2-thiophenecarboxylic acid. CAS Number: 444930-42-1. Molecular Formula: C17H14N2O2S. Formula Weight: 310.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 222, 289, 319, 333, 363 nm. SMILES: OC1=C(/C=N/NC(C2=C(C)C=CS2)=O)C=CC3=CC=CC=C31. InChi Code: InChI=1S/C17H14N2O2S/c1-11-8-9-22-16(11)17(21)19-18-10-13-7-6-12-4-2-3-5-14(12)15(13)20/h2-10,20H,1H3,(H,19,21)/b18-10+. InChi Key: NZWTWRNHYZNWNW-VCHYOVAHSA-N.