2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Wee1
  5. PKMYT1 Isoform

PKMYT1

PKMYT1 (protein kinase, membrane associated tyrosine/threonine 1) is a member of the WEE kinase family that functions as a key negative regulator of CDK1 activity and mitotic entry, thereby contributing to cell-cycle control and genomic stability[1][2]. Mechanistically, PKMYT1 participates in the G2/M checkpoint, where WEE-family kinases maintain inhibitory control over CDK1 to prevent premature progression into mitosis under conditions requiring cell-cycle surveillance[1][3]. Through this checkpoint-regulatory role, PKMYT1 supports proper mitotic timing and helps preserve genetic integrity in proliferating cells[1][3]. In cancer biology, increasing evidence indicates that tumor cells can become highly dependent on WEE-family kinase activity, including PKMYT1, to tolerate replication stress and DNA damage, making this pathway a relevant target for therapeutic investigation[1][3]. Studies in colorectal cancer have shown elevated PKMYT1 expression and demonstrated that PKMYT1 silencing impairs cellular proliferation, cell-cycle progression, migration, and invasion, supporting a role in tumor development and maintenance[4]. Compared with the related isoform WEE1, which has received substantially greater research attention, PKMYT1 remains a comparatively underexplored member of the WEE kinase family despite sharing critical functions in regulating mitotic control[5]. For experimental applications, PKMYT1 inhibitors have emerged as valuable tools for investigating G2/M checkpoint dependence, and inhibition of PKMYT1 can promote checkpoint override, premature mitotic entry, and mitotic cell death in cancer models, supporting its development as a potential therapeutic target[1][2].

PKMYT1 Related Products (27):

Cat. No. Product Name Effect Purity
  • HY-145817A
    lunresertib
    		Inhibitor 99.97%
    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.
  • HY-122113
    PD173952
    		Inhibitor 99.58%
    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 Ki of 8.1 nM. PD173952 induces apoptosis.
  • HY-145817
    (Rac)-lunresertib
    		Inhibitor 99.72%
    (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.
  • HY-170517
    PKMYT1-IN-8
    		Inhibitor 99.31%
    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.
  • HY-145664
    Myt1-IN-1
    		Inhibitor 98.97%
    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).
  • HY-180485
    PROTAC D16-M1P2
    		Degrader
    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.
  • 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).
  • 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.
  • HY-145817B
    (R)-lunresertib
    		Inhibitor 99.87%
    (R)-lunresertib is a membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor, with IC50 of 1360 nM. (R)-lunresertib can be used in the study of Myt1-mediated cancers.
  • HY-145666
    Myt1-IN-3
    		Inhibitor 99.14%
    Myt1-IN-3 is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC50s of <10 nM (WO2021195782 A1, compound 95).
  • HY-163490
    PKMYT1-IN-1
    		Inhibitor 99.24%
    PKMYT1-IN-1 (Compound 1) is an inhibitor for membrane-associated tyrosine and threonine kinase (PKMYT1), with an IC50 of 8.8 nM. PKMYT1-IN-1 inhibits proliferation of tumor cell HCC1569 with IC50 of 42 nM.
  • HY-169946
    WEE1/PKMYT1-IN-1
    		Inhibitor 98.84%
    WEE1/PKMYT1-IN-1 (compound 75) is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.
  • HY-145665
    Myt1-IN-2
    		Inhibitor
    Myt1-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).
  • HY-172759
    PKMYT1-IN-9
    		Inhibitor
    PKMYT1-IN-9 is a highly selective and orally active PKMYT1 inhibitor (IC50: 4.4 nM). PKMYT1-IN-9 shows more selective for PKMYT1 than WEE1 (IC50: 32.4 μM). PKMYT1-IN-9 exhibits antitumor activity.
  • HY-163491
    PKMYT1-IN-2
    		Inhibitor
    PKMYT1-IN-2 (compound 2) is a potent PKMYT1 inhibitor with an IC50 of 5.7 nM. PKMYT1-IN-2 inhibits the growth of HCC1569 cells with an IC50 of 22 nM.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.