GRN-300

GRN-300 (also known as ARN-3261) is an orally bioavailable, first-in-class small molecule inhibitor that targets salt-inducible kinase 2 and 3 (SIK2 and SIK3). By inhibiting these serine/threonine kinases, which are overexpressed in a significant proportion of ovarian cancer specimens, GRN-300 disrupts pathways involved in DNA repair and apoptosis. Preclinical studies have shown that SIK2/3 inhibition by GRN-300 sensitizes ovarian and breast cancer cells to PARP inhibitors such as olaparib and enhances the efficacy of standard chemotherapies like paclitaxel. The drug is being developed for the treatment of advanced solid tumors including ovarian cancer and triple-negative breast cancer. Its mechanism may help overcome chemoresistance in these cancers[1][2][3][4][5].

Other names

GRN 300GRN300GRN-300ARN3261ARN-3261ARN 3261