444930-42-1
Chemical Structure
PCNA-I1
- CAS No.: 444930-42-1
- Formula:C17H14N2O2S
- Molecular Weight:310.37
IUPAC Name: (E)-N'-((1-hydroxynaphthalen-2-yl)methylene)-3-methylthiophene-2-carbohydrazide
InChIKey: NZWTWRNHYZNWNW-VCHYOVAHSA-N
SMILES: O=C(N/N=C/C1=C(C2=CC=CC=C2C=C1)O)C3=C(C=CS3)C
Biological Activity: PCNA-I1 is a selective small molecule inhibitor targeting proliferating cell nuclear antigen (PCNA) with anticancer activity. PCNA-I1 can stabilize the PCNA trimer structure (Kd=0.14-0.41μM), reduce its binding to chromatin, induce tumor cell cycle arrest, inhibit DNA replication and repair, and enhance the anti-tumor effect of DNA damaging agents. PCNA-I1 can be used in the study of targeted therapy for prostate cancer, lung cancer and other tumors[1][2][3].
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PCNA-I1 | 98.78% | PCNA-I1 is a selective small molecule inhibitor targeting proliferating cell nuclear antigen (PCNA) with anticancer activity. PCNA-I1 can stabilize the PCNA trimer structure (Kd=0.14-0.41μM), reduce its binding to chromatin, induce tumor cell cycle arrest, inhibit DNA replication and repair, and enhance the anti-tumor effect of DNA damaging agents. PCNA-I1 can be used in the study of targeted therapy for prostate cancer, lung cancer and other tumors. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Lu S, et al. Additive effects of a small molecular PCNA inhibitor PCNA-I1S and DNA damaging agents on growth inhibition and DNA damage in prostate and lung cancer cells. PLoS One. 2019 Oct 10;14(10):e0223894. [Content Brief]
- [3]. Dillehay KL, et al. Antitumor effects of a novel small molecule targeting PCNA chromatin association in prostate cancer. Mol Cancer Ther. 2014 Dec;13(12):2817-26. [Content Brief]
Keywords
