2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Wee1

Wee1

Wee1

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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 Isoform Specific Products:

Wee1 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169946A
    WEE1/PKMYT1-IN-2
    		Inhibitor
    WEE1/PKMYT1-IN-2 is the axial chiral P configuration of WEE1/PKMYT1-IN-1 (HY-169946). WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.
    WEE1/PKMYT1-IN-2
  • HY-175817
    PKMYT1-IN-10
    		Inhibitor
    PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.
    PKMYT1-IN-10
  • HY-133703A
    i-AZD1775 TFA
    		Inhibitor
    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.
    i-AZD1775 TFA
  • HY-161879
    WEE1-IN-9
    		Inhibitor
    WEE1-IN-9 (Compound 1) is a Wee1 inhibitor that can be used in cancer research.
    WEE1-IN-9
  • HY-160530
    WEE1-IN-6
    		Inhibitor
    WEE1-IN-6 (compound 110) is a orally active WEE1 inhibitor with an DC50 value of ≦ 100 nM. WEE1-IN-6 inhibits cell proliferation.
    WEE1-IN-6
  • HY-175261
    DHI1
    		Inhibitor
    DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies.
    DHI1
  • HY-172807
    p38α-IN-9
    		Inhibitor
    p38α-IN-9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC50 lower than 20 nM. p38α-IN-9 inhibits MK2T334 phosphorylation. p38α-IN-9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α-IN-9 Inhibits colorectal cancer (CRC) metastasis.
    p38α-IN-9
  • HY-169946B
    WEE1/PKMYT1-IN-3
    		Inhibitor
    WEE1/PKMYT1-IN-3 is the axial chiral M configuration of WEE1/PKMYT1-IN-1 (HY-169946). WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.
    WEE1/PKMYT1-IN-3
  • HY-180484
    PKMYT1-IN-12
    		Inhibitor
    PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2 (HY-180485).
    PKMYT1-IN-12
  • HY-175819
    PD-166285
    		Inhibitor
    PD-166285 is a PKMYT1 inhibitor, with an IC50 value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC50 = 0.14 μM) and HCC1569 cells (IC50 = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers.
    PD-166285
  • HY-13925A
    PD0166285 dihydrochloride
    		Inhibitor
    PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1.
    PD0166285 dihydrochloride
  • HY-143340
    LEB-03-145
    LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker.
    LEB-03-145
  • HY-182790
    BAA-065
    		Inhibitor
    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.
    BAA-065
  • HY-183547
    WEE1/PKMYT1-IN-4
    		Inhibitor
    WEE1/PKMYT1-IN-4 is a selective WEE1/PKMYT1 inhibitor, with IC50 values of 0.185 μM and 2.2 nM for human WEE1 and PKMYT1, respectively. WEE1/PKMYT1-IN-4 inhibits phosphorylation of CDK1 at T14 and Y15, disrupting the G2/M cell cycle checkpoint. WEE1/PKMYT1-IN-4 can be used for the research of colorectal cancer and amplified breast cancer.
    WEE1/PKMYT1-IN-4
  • HY-183278
    APO-50815
    		Inhibitor
    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.
    APO-50815
  • HY-161871
    WEE1-IN-8
    		Inhibitor
    WEE1-IN-8 (Compound 55) is a selective WEE1 inhibitor, with an IC50 of 0.98 nM. WEE1-IN-8 (Compound 55) can be used for the research of Pancreatic cancer, Ovarian cancer, Colorectal cancer, Uterine serous carcinoma, etc.
    WEE1-IN-8
  • HY-176363
    Adavosertib-C3-NH-Boc
    		Inhibitor
    Adavosertib-C3-NH-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for Wee1 (HY-10993) and a PROTAC linker (HY-W011561), which recruits E3 ligases. Adavosertib-C3-NH-Boc can be used for synthesis of PROTAC Pomalidomide-C3-adavosertib (HY-133618).
    Adavosertib-C3-NH-Boc
  • HY-176957
    PKMYT1-IN-11
    		Inhibitor
    PKMYT1-IN-11 (Example 1) is a PKMYT1 inhibitor with an IC50 of 4.49 nM. PKMYT1-IN-11 inhibits the proliferation of HCC1569 cells. When combined with Gemcitabine (HY-17026), PKMYT1-IN-11 shows a significant anti-tumor effect in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 can be used for the study of various cancers such as breast cancer and ovarian cancer.
    PKMYT1-IN-11
  • HY-162849
    PKMYT1-IN-3
    		Inhibitor
    PKMYT1-IN-3 (compound 8ma) is a potent and selective PKMYT1 inhibitor with an IC50 value of 16.5 nM. PKMYT1-IN-3 has antitumor activity.
    PKMYT1-IN-3
  • HY-182433
    CJM061
    		Inhibitor
    CJM061 is a WEE1 kinase inhibitor with a target IC50 of 2.8 nM. CJM061 acts as a sensitizer and exhibits synergistic effects with Cisplatin (HY-17394) in medulloblastoma cells. CJM061 can be used for the research of medulloblastoma.
    CJM061
Wee1 Isoform Comparison

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