IAG-10 is a selective DNA polymerase kappa ( hpol κ ) inhibitor with an IC50 value of 7.2 μM. IAG-10 exerts its function by disrupting the formation of the binary complex between the enzyme and DNA. IAG-10 enhances the antiproliferative and DNA-damaging activities of Temozolomide in tumor cells with functional hpol κ expression. IAG-10 can be used in the research of cancers such as malignant brain tumors [1].
In Vitro, IAG-10 (0.1-0.5 μM; 1 hour) potentiates the anti-proliferative effect of Temozolomide in hpol κ-proficient HAP-1 cells but not in hpol κ-deficient cells, indicating target-dependent activity[1]. IAG-10 (0.5 μM; 1 hour) increases DNA damage in hpol κ-proficient HAP-1 cells alone and in combination with Temozolomide, with no effect in hpol κ-deficient cells[1].
References:
[1]. Ketkar A, et al. Inhibition of Human DNA Polymerases Eta and Kappa by Indole-Derived Molecules Occurs through Distinct Mechanisms. ACS Chem Biol. 2019;14(6):1337-1351.
In Vitro, IAG-10 (0.1-0.5 μM; 1 hour) potentiates the anti-proliferative effect of Temozolomide in hpol κ-proficient HAP-1 cells but not in hpol κ-deficient cells, indicating target-dependent activity[1]. IAG-10 (0.5 μM; 1 hour) increases DNA damage in hpol κ-proficient HAP-1 cells alone and in combination with Temozolomide, with no effect in hpol κ-deficient cells[1].
References:
[1]. Ketkar A, et al. Inhibition of Human DNA Polymerases Eta and Kappa by Indole-Derived Molecules Occurs through Distinct Mechanisms. ACS Chem Biol. 2019;14(6):1337-1351.