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G2M checkpoint

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13902
    Berzosertib
    Maximum Cited Publications
    24 Publications Verification

    VE-822; VX-970; M6620

    ATM/ATR Apoptosis STING Caspase Infection Metabolic Disease Cancer
    Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
    Berzosertib
  • HY-19959
    Mirin
    5+ Cited Publications

    ATM/ATR Apoptosis Cancer
    Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .
    Mirin
  • HY-15883

    Checkpoint Kinase (Chk) Apoptosis Cancer
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
    GNE-900
  • HY-178190

    Wee1 Cancer
    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-13
  • HY-146792

    Polo-like Kinase (PLK) Cancer
    PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
    PLK1-IN-4
  • HY-112347

    Checkpoint Kinase (Chk) Cancer
    Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response .
    Isogranulatimide
  • HY-156916

    Microtubule‐associated serine/threonine kinase (MAST) Metabolic Disease
    WAY-230563 (ST045945) is a serine/threonine kinase inhibitor that can block CHK1/CHK2-mediated cell cycle checkpoints. WAY-230563 can induce G2/M phase arrest and DNA damage in tumor cells .
    ST045945
  • HY-178150

    Wee1 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-14
  • HY-168739

    Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis Cancer
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
    Topoisomerase I inhibitor 17
  • HY-160948

    Wee1 Checkpoint Kinase (Chk) Cancer
    DB07006 (compound 18) is a potent, ATP-cpmpetitive dual inhibitor of Wee1 (IC50 = 0.030 μM) and Chk1 checkpoint kinases (IC50 = 0.018 μM). DB07006 demonstrates effective abrogation of the G2/M checkpoint in combination with DNA-damaging agents in cellular models. DB07006 can be used for cancer research .
    DB07006
  • HY-108343R

    Reference Standards Wee1 Cancer
    WEE1-IN-4 (Standard) is the analytical standard of WEE1-IN-4 (HY-108343). This product is intended for research and analytical applications. WEE1-IN-4 (Compound 15) is a potent checkpoint Wee1 Kinase inhibitor with an IC50 of 0.011 μM. Wee1 inhibitors can abrogate the G2/M checkpoint .
    WEE1-IN-4 (Standard)
  • HY-13902A
    Berzosertib hydrochloride
    Maximum Cited Publications
    24 Publications Verification

    VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride

    ATM/ATR Apoptosis STING Caspase Neurological Disease Cancer
    Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
    Berzosertib hydrochloride
  • HY-183547

    Wee1 CDK Cancer
    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-183118

    CDK Apoptosis Neurological Disease Cancer
    CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
    CID-078
  • HY-W851050A

    PDI Neurological Disease Cancer
    BAP2 is an allosteric protein disulfide isomerase (PDI) inhibitor with a IC50 of 0.85 μM. BAP2 binds to His256 in the b′ domain of PDI and exerts inhibitory effects through allosteric binding to the b′ domain. BAP2 upregulates GRP78. BAP2 inhibits the growth of glioblastoma cells. BAP2 can be used in studies related to glioblastoma .
    BAP2

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