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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA Repair Protein -PCNA-I1
PCNA-I1

Chemical Structure : PCNA-I1

CAS No.: 444930-42-1

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PCNA-I1 (PCNA inhibitor 1)

货号: PC-38448Not For Human Use, Lab Use Only.

PCNA-I1 is a small molecule inhibitor of proliferating cell nuclear antigen (PCNA), selectively binds to PCNA trimers with Kd of 0.14-0.41 uM, inhibits the growth of tumor cells of various tissue types with IC50 of 0.2 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PCNA-I1 is a small molecule inhibitor of proliferating cell nuclear antigen (PCNA), selectively binds to PCNA trimers with Kd of 0.14-0.41 uM, inhibits the growth of tumor cells of various tissue types with IC50 of 0.2 uM.
PCNA-I1 dose- and time-dependently reduced the chromatin-associated PCNA in cells, affected the growth of nontransformed cells at significantly higher concentrations (IC50=1.6 uM).
PCNA-I1 also dose-dependently reduced uptake of BrdU in PCNA-I1 treated cells, induced cancer cell arrest at both the S and G(2)/M phases.
PCNA-I1 induced DNA damage and apoptosis in both LNCaP (wild-type p53) and PC-3 cells (p53-null) and enhanced DNA damage and apoptosis triggered by cisplatin, also induced autophagy in PC-3 cells.
PCNA-I1 (i,v.) significantly retarded growth of LNCaP tumors of in nude mice without causing detectable effects on mouse body weight and hematology profiles.

物理化学性质&存储条件

分子量 310.37
分子式 C17H14N2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Thiophenecarboxylic acid, 3-methyl-, 2-[(1-hydroxy-2-naphthalenyl)methylene]hydrazide

参考文献

1. Tan Z, et al. Mol Pharmacol. 2012 Jun;81(6):811-9.

2. Dillehay KL, et al. Mol Cancer Ther. 2014 Dec;13(12):2817-26.

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