WSD0628

WSD0628 is a potent, selective, orally bioavailable small molecule inhibitor of ataxia telangiectasia mutated (ATM) kinase. It was specifically designed to penetrate the blood-brain barrier and acts as a radiosensitizer for glioblastoma (GBM) and metastatic central nervous system (CNS) tumors. By inhibiting ATM kinase—a key regulator of DNA double-strand break repair—WSD0628 suppresses DNA repair mechanisms and checkpoint controls in tumor cells, thereby enhancing the efficacy of radiation therapy and potentially other DNA-damaging chemotherapies. Preclinical studies demonstrate that WSD0628 increases radiosensitivity in GBM, melanoma brain metastases, and astrocytes; it shows robust CNS penetration with minimal efflux transporter liability. Clinical development is ongoing for its use in combination with radiation therapy for GBM and brain metastases[1][2][3][4][5][6][7][8].

Other names

ATM kinase inhibitor WSD-0628