A83B4C63

A83B4C63 is a potent, small molecule inhibitor of the DNA repair enzyme polynucleotide kinase 3'-phosphatase (PNKP). It was developed as a lead compound for targeting DNA repair pathways in cancer, particularly for use as a radiosensitizer and chemosensitizer in PTEN-deficient colorectal cancer. The drug exhibits high affinity for PNKP (Kd = 80 nM) and has shown efficacy in preclinical models by sensitizing tumor cells to DNA-damaging therapies such as radiation. Due to its poor water solubility, nano-encapsulated formulations have been developed to enhance delivery and reduce toxicity to normal tissues. Preclinical studies demonstrated significant survival extension and enhanced tumor growth delay when combined with radiation therapy, without notable toxicity to healthy tissues[1][3][5].

Other names

PNKP inhibitor