Wee1 Degrader

BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research.

Pomalidomide-C3-adavosertib is a rapid and selective PROTAC Wee1 degrader (IC₅₀=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis.

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.

HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC₅₀: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker).

PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC₅₀ of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC₅₀ of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC₅₀ of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer.