Wee1
Wee1 is a nuclear kinase belonging to the Ser/Thr family of protein kinases in the fission yeast Schizosaccharomyces pombe (S. pombe). Wee1 has amolecular mass of 96 kDa and it is a key regulator of cell cycle progression. Wee1 influences cell size by inhibiting the entry into mitosis, through inhibiting Cdk1. Wee1 has homologues in many other organisms, including mammals. Wee1 inhibits Cdk1 by phosphorylating it on two different sites, Tyr15 and Thr14. Cdk1 is crucial for the cyclin-dependent passage of the various cell cycle checkpoints. At least three checkpoints exist for which the inhibition of Cdk1 by Wee1 is important: G2/M checkpoint, Cell size checkpoint, DNA damage checkpoint. Wee1 is shown to phosphorylate histone H2B at tyrosine 37 residue which regulates global expression of histones.
WEE1 subfamily includes PMYT1.
WEE1 subfamily includes PMYT1.
Wee1 Isoform Specific Products
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Wee1 Related Products (82)
Related Products (82)
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Wee1 Isoform Comparison
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PKMYT1-IN-8
0 ImagesPKMYT1-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.
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HEMTAC WEE1 degrader-1
0 ImagesHEMTAC 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).
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WEE1-IN-3
0 ImagesWEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities.
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Myt1-IN-1
0 ImagesMyt1-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).
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WEE1-IN-10
0 ImagesCat. No.: HY-161880CAS No.: 2226938-19-6
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PDK1-IN-1
0 ImagesPDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor. PDK1-IN-1 is also useful as inhibitor of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. PDK1-IN-1 selectively inhibits microtubule affinity regulating kinase (MARK). PDK1-IN-1 can be used for researches of myeloproliferative disorders, cancer and Alzheimer's disease.
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PROTAC D16-M1P2
0 ImagesCat. No.: HY-180485PROTAC D16-M1P2 is an orally active CRBN-mediated selective PKMYT1 PROTAC degrader, with a DC50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells. PROTAC D16-M1P2 induces PKMYT1 degradation via the ubiquitin-proteasome system, directly inhibits PKMYT1 kinase activity, suppresses Thr14 phosphorylation of CDK1, and depends on functional CRBN and ubiquitination-like modification processes. PROTAC D16-M1P2 can be used for the research of CCNE1-amplified breast cancer, FBXW7-mutated cholangiocarcinoma, and PPP2R1A-deficient cancers.
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Myt1-IN-2
0 ImagesCat. No.: HY-145665CAS No.: 2719748-43-1Myt1-IN-2 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-2 has anticancer effects (WO2021195782A1; compound 28).
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XL495
0 ImagesCat. No.: HY-182906CAS No.: 3040320-93-9XL495 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.
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WEE1-IN-13
0 ImagesCat. No.: HY-178190WEE1-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).
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WEE1-IN-14
0 ImagesCat. No.: HY-178150CAS No.: 2803921-87-9WEE1-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.
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WEE1-IN-12
0 ImagesCat. No.: HY-174448CAS No.: 3069940-37-7WEE1-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.
