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G2-M 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
    GNE-900

    		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-IN-13

    		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
    PLK1-IN-4

    		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-178150
    WEE1-IN-14

    		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-112347
    Isogranulatimide

    		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
    ST045945

    		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-168739
    Topoisomerase I inhibitor 17

    		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
    DB07006

    		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
    WEE1-IN-4 (Standard)

    		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/PKMYT1-IN-4

    		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
    CID-078

    		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

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