Catalog No.: PC-24377Not For Human Use, Lab Use Only.
WSD0628 (WSD-0628) is a potent, selective, orally bioavailable and CNS penetrant ATM inhibitor, potently inhibits ATM-mediated phosphorylation of the DNA damage response protein KAP1 in MCF-7 cells with IC50 of 0.42 nM.
WSD0628 (WSD-0628) is a potent, selective, orally bioavailable and CNS penetrant ATM inhibitor, potently inhibits ATM-mediated phosphorylation of the DNA damage response protein KAP1 in MCF-7 cells with IC50 of 0.42 nM.
WSD0628 is much less potent inhibition of the related kinases ATR (phosphorylation of CHK1, IC50 742nM) or DNA-PKcs (auto-phosphorylation of DNA-PK, IC50 169nM) in HT29 cells.
WSD-0628 (30 nM) potently inhibited RT-induced phospho-KAP1 and robustly reduced clonogenic survival by 5-fold when combined with 5 Gy irradiation in U251 GBM cells.
WSD0628 is orally bioavailable and CNS penetrant without efflux transporter liability.
2. Tuma, A. M. et al. Abstract 3305: WSD-0628, a novel brain penetrant ATM inhibitor, radiosensitizes GBM and melanoma patient derived xenografts. Cancer Res. 2022, 82, 3305– 3305.
