7-Methylguanine

7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a K_i value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions^{[1][2][3][4][5][6]}. In Vitro:7-Methylguanine (0-200 μM) inhibits PARP1 enzymatic activity in a dose-dependent manner^[1].
7-Methylguanine is a competitive PARP-1 inhibitor with a K_i value of 61 μM^[2].
7-Methylguanine (0-450 μM) inhibits the dissociation of the PARP-1-DNA complex due to suppression of PARP-1 catalytic activity^[2].
7-Methylguanine (0.02-0.2 mg/mL; 24 h) does not produce DNA damage in immortalized human kidney epithelial cells (NKE-hTERT)^[3].
In Vivo:7-Methylguanine (50 mg/kg; p.o..; 3 times per week; 4 weeks for toxicology study) exerts no adverse effects or changes in morphology in CBA, BALB/c, and C57BL/6 mice as well as inhibits tumor growth in CBA mice with uterine sarcoma US-322^[3].
7-Methylguanine (50 mg/kg; i.g.; 3 times per week) effectively penetrates tumor tissue and suppresses colon adenocarcinoma growth in BALB/c mice with transplanted Akatol tumor^[5].