WEE1 degrader 1 (Compound 10) is a CRBN -dependent molecular glue degrader of WEE1 and casein kinase 1α ( CK1α ) with sub-2 nM DC50 values for both targets. WEE1 degrader 1 can be used for the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, diffuse large b cell lymphoma [1].
In Vitro, WEE1 degrader 1 (tested concentrations; 5 h) potently induces degradation of both CK1α and WEE1 in Jurkat cells, with sub-2 nM DC50 values and near-complete WEE1 degradation[1]. WEE1 degrader 1 (1 μM; 5 h) potently degrades both WEE1 and CK1α in a broad panel of human hematological and solid tumor cell lines when treated at 1 μM for 5 h[1]. WEE1 degrader 1 (range of concentrations; 72 h) potently inhibits proliferation of multiple human cancer cell lines, with near-complete cell death at 10 μM and EC50 values indicating strong cytotoxicity[1].
References:
[1]. Razumkov H, et al. Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library. J Am Chem Soc. 2024;146(46):31433-31443.
In Vitro, WEE1 degrader 1 (tested concentrations; 5 h) potently induces degradation of both CK1α and WEE1 in Jurkat cells, with sub-2 nM DC50 values and near-complete WEE1 degradation[1]. WEE1 degrader 1 (1 μM; 5 h) potently degrades both WEE1 and CK1α in a broad panel of human hematological and solid tumor cell lines when treated at 1 μM for 5 h[1]. WEE1 degrader 1 (range of concentrations; 72 h) potently inhibits proliferation of multiple human cancer cell lines, with near-complete cell death at 10 μM and EC50 values indicating strong cytotoxicity[1].
References:
[1]. Razumkov H, et al. Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library. J Am Chem Soc. 2024;146(46):31433-31443.