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Cat. No. Product Name CAS No. Information
PC-35301

AOH1160

2089314-57-6

AOH1160 (AOH-1160) is a potent, first-in-class, orally available small molecule inhibitor of Proliferating cell nuclear antigen (PCNA); selectively kills many types of cancer cells at below micromolar concentrations (mean GI50=330 nM) without causing significant toxicity to a broad range of non-malignant cells, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, and causes cell cycle arrest; suppresses tumor growth without causing significant side effects in mice, demostrates the potential as a broad-spectrum therapeutic agent for cancer treatment.

PC-63192

IACS-4619

1884209-98-6

IACS-4759 potent, selective aminopyrimidine MTH1 (MutT homolog 1) inhibitor with IC50 of 0.2 nM; shows no off-target kinase activity in a panel of 97 kinases; exhibits excellent cell permeability and good metabolic stability in microsomes; an excellent tool for interrogation of the utility of MTH1 inhibition in the context of oncology.

PC-62706

Karonudib

Karonudib (TH1579) is an analogue of TH588, a potent, selective MTH1 inhibitor with good oral availability and demonstrates excellent pharmacokinetic and anti-cancer properties in vivo.

Solid Tumors

Phase 1 Clinical

PC-62705

IACS-4759

1884209-99-7

IACS-4759 potent, selective aminopyrimidine MTH1 (MutT homolog 1) inhibitor with IC50 of 0.6 nM; shows no off-target kinase activity in a panel of 97 kinases; exhibits excellent cell permeability and good metabolic stability in microsomes; an excellent tool for interrogation of the utility of MTH1 inhibition in the context of oncology.

PC-62517

TH 5427

TH 5427 (TH5427) is a potent, small molecule NUDT5 (NUDIX5) inhibitor with IC50 of 29 nM, 690-fold selectivity for NUDT5 over MTH1 (NUDT1) in vitro; shows little to no effect on NUDT9, dCTPase, NUDT12 and NUDT14; inhibits progestin-dependent nuclear ATP synthesis, subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells; a potent NUDT5 inhibitor that blocks hormone-dependent gene expression in breast cancer cells.

PC-62268

YU 238259

1943733-16-1

YU 238259 is a novel DNA double-strand break repair inhibitor that exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects; specifically inhibits homology-dependent DNA repair (HDR), but not non-homologous end-joining (NHEJ), in cell-based GFP reporter assays; significantly delays tumor growth of BRCA2-deficient human tumor xenografts in nude mice.

PC-61928

D-I03

688342-78-1

D-I03 (D-103) is a small molecule that inhibits RAD52-mediated ssDNA annealing with IC50 of 5 uM, binds to RAD52 with Kd of 25.8 uM and inhibits D-loop formation with IC50 of 8 uM in vitro; suppresses growth of BRCA1- and BRCA2-deficient cells (at 2.5 uM concentration) and inhibits RAD52-mediated SSA in human U2OS cells; selective toward SSA over homologous recombination (HR).

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