| Hazard Information | Back Directory | [Description]
PNR-7-02 is an inhibitor of human DNA polymerase eta (Polη). | [Uses]
PNR-7-02 inhibits Pol η function with an IC50 value of near 8 μM, which binds to the little finger domain. PNR-7-02 is also an inhibitor against hRev1 and hpol lambda (λ). PNR-7-02 acts synergistically with Cisplatin (HY-17394) to kill chronic myeloid leukaemia and ovarian cancer cell lines. PNR-7-02 is an indole thio-barbituric acid (ITBA) derivative with both N-napthoyl moiety and 5-chloro substituent on the indole ring[1][2]. | [References]
[1] Zafar M K, et al. Investigation of Structure‐Activity Relationships for Small‐Molecule Inhibitors of Human DNA Polymerase Eta[J]. The FASEB Journal, 2016, 30: 1052.3-1052.3.
[2] Ler AAL, et al. DNA Damage Tolerance Pathways in Human Cells: A Potential Therapeutic Target. Front Oncol. 2022 Feb 7;11:822500. DOI:10.3389/fonc.2021.822500 |
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