Wee1 Inhibitor

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

lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC₅₀ of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects.

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.

XL495 is an potent, selective and orally active PKMYT1 inhibitor. XL495 inhibits CDK1 Thr14 phosphorylation and induces KAP1 Ser824 phosphorylation in xenograft tumors. XL495 reduces tumor growth in colorectal and breast cancer xenograft models, and achieves tumor regression with DNA-damaging agents in colorectal cancer xenograft models. XL495 can be used for the research of cancer, such as breast cancer and colorectal cancer.

BAA-065 is a selective and orally active PKMYT1 inhibitor with an IC₅₀ of <50 nM. BAA-065 inhibits cancer cells proliferation, induces γH2AX expression and DNA damage. BAA-065 inhibits tumor growth in OVCAR3 xenograft mice. BAA-065 can be used for the research of cancer, such as ovarian 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.

PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC₅₀s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.

PD173952 is a tyrosine kinases inhibitor with IC₅₀s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a K_i of 8.1 nM. PD173952 induces apoptosis.

FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.

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.

(Rac)-lunresertib (compound 181) is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀ of <10 nM. (Rac)-lunresertib (compound 181) has anticancer effects.

PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC₅₀ of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC₅₀s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI₅₀ of 2.02 μM.

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

Myt1-IN-1 is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀ of <10 nM. Myt1-IN-1 has anticancer effects (WO2021195782A1; compound 132).

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.