PCNA-I1 是一种有效的 PCNA(增殖细胞核抗原)抑制剂。 PCNA-I1 直接结合 PCNA 三聚体,Kd 为 0.41 μM,并在体外和体内均表现出抗肿瘤活性。
Cas No. | 444930-42-1 |
Canonical SMILES | OC1=C(/C=N/NC(C2=C(C)C=CS2)=O)C=CC3=CC=CC=C31 |
分子式 | C17H14N2O2S |
分子量 | 310.4 |
溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. |