Wee1 Inhibitor

Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC₅₀ of 5.2 nM.

Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC₅₀=3.9 nM). Azenosertib exhibits antitumor activity.

PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 exhibits an IC₅₀ of 3.433 μM for Chk1.

Zedoresertib (Debio 0123) is a potent WEE1 inhibitor with an IC₅₀ value of 0.8 nM. Zedoresertib inhibits phospho-CDC2. Zedoresertib abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. Zedoresertib can be used for researching anticancer.

Surbinsertib (SGR-3515) is an orally active dual inhibitor of the Wee1 and Myt1 kinases. Surbinsertib is used in cancer research.

APO-50815 is a WEE1 kinase inhibitor with a human IC₅₀ of 9 nM. APO-50815 induces DNA damage, replication stress, S-phase cell accumulation, and apoptosis. APO-50815 can be used for the research of metastatic colorectal cancer.

Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.

GSK-1520489A is a PKMYT1 (active protein kinase) inhibitor (IC₅₀=115 nM, K_i=10.94 nM).

WEE1-IN-4 (compound 15) is a pyrrolocarbazole-1,3(2H,6H)-dione derivative and Wee1 kinase inhibitor with an IC₅₀ value of 11 nM.WEE1-IN-4 can be used for the research of cancer.

Bosutinib isomer is a ligand or inhibitor with high binding affinity for both Wee1 and Wee2, with K_d values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively.

WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC₅₀ of <10 nM. WEE1-IN-3 has anticancer activities.

WEE1-IN-10 (compound 77) is a Wee1 kinase inhibitor. WEE1-IN-10 shows inhibitory activity on LOVO cell growth, with an IC₅₀ of 0.524 μM. WEE1-IN-10 can be used for the research of diseases caused by abnormal activity of Wee1.

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC₅₀ value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity.

Adavosertib (Standard) is the analytical standard of Adavosertib. This product is intended for research and analytical applications. Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC₅₀ of 5.2 nM.

WEE1-IN-13 (Compound 10) is a highly selective WEE1 kinase inhibitor (IC₅₀=0.7 nM). WEE1-IN-13 abrogates the G2/M checkpoint and induces tumor cell apoptosis. WEE1-IN-13 is promising for research of solid tumors (e.g., non-small cell lung cancer, ovarian cancer).

WEE1-IN-14 (Compound 14) is a selective WEE1 inhibitor (IC₅₀: 0.5 nM in L-RB-FEP calculations, 1.0 nM in ADP-Glo kinase assay). Inhibition of Wee1 in cancer cells disrupts the G2-M checkpoint, removes the regulatory controls on the cell cycle, and leads to early onset of mitotic failure followed by apoptosis of tumor cells. Therefore, WEE1-IN-14 is a useful tool for studying cancer biology.

WEE1-IN-12 (Compound 87) is a Wee1 kinase inhibitor with an IC₅₀ of 2.0 nM. WEE1-IN-12 can inhibit the proliferation of HT29 cells (IC₅₀: 1.07 μM), and when used in combination with Gemcitabine (HY-17026), the effect is better (IC₅₀: 0.34 μM). WEE1-IN-12 can be used in the research of tumors such as colon cancer.

i-AZD1775 TFA is a Target Protein Ligand-Linker Conjugate that contains a target protein ligand and a PROTAC linker, and can recruit E3 ligases. i-AZD1775 TFA can be used for the synthesis of Pomalidomide-C3-adavosertib (HY-133618). i-AZD1775 TFA is an immobilizable analogue of AZD1775. i-AZD1775 TFA retains the ability to inhibit WEE1 in vitro. i-AZD1775 TFA can be studied in anticancer research.

WEE1-IN-9 (Compound 1) is a Wee1 inhibitor that can be used in cancer research.

WEE1-IN-6 (compound 110) is a orally active WEE1 inhibitor with an DC₅₀ value of ≦ 100 nM. WEE1-IN-6 inhibits cell proliferation.