Polθ-IN-9 is a selective inhibitor of Pol θ polymerase, demonstrating an IC50 value of 9.6 nM and a Kd of 47.5 nM, with no significant inhibitory effects on other human DNA polymerases such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. This compound exhibits potent antiproliferative activity in DLD1 BRCA2 knockout cells (IC50 = 2.9 μM) and MDA-MB-436 cells (IC50 = 4.9 μM), while also increasing DNA damage and γH2AX levels. In addition, Polθ-IN-9 has shown to inhibit tumor growth in conjunction with Olaparib in the MDA-MB-436 xenograft model, making it a valuable tool for studying homologous recombination-deficient cancers, including breast cancer.
Polθ-IN-9 is a selective inhibitor of Pol θ polymerase, demonstrating an IC50 value of 9.6 nM and a Kd of 47.5 nM, with no significant inhibitory effects on other human DNA polymerases such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. This compound exhibits potent antiproliferative activity in DLD1 BRCA2 knockout cells (IC50 = 2.9 μM) and MDA-MB-436 cells (IC50 = 4.9 μM), while also increasing DNA damage and γH2AX levels. In addition, Polθ-IN-9 has shown to inhibit tumor growth in conjunction with Olaparib in the MDA-MB-436 xenograft model, making it a valuable tool for studying homologous recombination-deficient cancers, including breast cancer.
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