| Identification | Back Directory | [Name]
PCNA-I1 | [CAS]
444930-42-1 | [Synonyms]
2-Thiophenecarboxylic acid, 3-methyl-, 2-[(1-hydroxy-2-naphthalenyl)methylene]hydrazide
N-(3-Methylthiophene-2-carboxylic acid)-N'-[(1-hydroxy-2-naphthalenyl)methylene]hydrazide | [Molecular Formula]
C17H14N2O2S | [MOL File]
444930-42-1.mol | [Molecular Weight]
310.37 |
| Chemical Properties | Back Directory | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | [form ]
A crystalline solid | [pka]
8.31±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
PCNA-I1 is a potent PCNA (proliferating cell nuclear antigen) inhibitor. PCNA-I1 directly binds PCNA trimers with a Kd of 0.41 μM and exhibits antitumor activity both in vitro and in vivo[1]. | [storage]
Store at -20°C | [References]
[1] Tan Z, et al. Small-molecule targeting of proliferating cell nuclear antigen chromatin association inhibits tumor cell growth. Mol Pharmacol. 2012 Jun;81(6):811-9. DOI:10.1124/mol.112.077735 |
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