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PCNA-I1

Chemical Structure : PCNA-I1

CAS No.: 444930-42-1

PCNA-I1 (PCNA inhibitor 1)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 310.37
Formula C17H14N2O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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