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Pathways Recommended: Cell Cycle/DNA Damage Stem Cell/Wnt
Results for "

cell cycle checkpoint

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

1

Screening Libraries

1

Biochemical Assay Reagents

1

Peptides

4

Antibodies

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W011425
    NTPO

    Nitrilotris(methylenephosphonic acid)

    		 DNA Alkylator/Crosslinker Cancer
    NTPO (Nitrilotris methylenephosphonic acid) is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
    NTPO
  • HY-124955
    proTAME
    Maximum Cited Publications
    6 Publications Verification

    		 APC Cancer
    proTAME, a cell-permeable proagent form of TAME, is an anaphase promoting complex/cyclosome (APC/C) inhibitor. proTAME causes cell cycle arrest in metaphase .
    proTAME
  • HY-107407
    SB-218078
    5 Publications Verification

    		 Checkpoint Kinase (Chk) CDK PKC Apoptosis Cancer
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
    SB-218078
  • 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-142931
    ATM-IN-1

    		ATM/ATR Neurological Disease Cancer
    ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3) .
    ATM-IN-1
  • HY-174543
    Human PRKCA mRNA

    		mRNA Cancer
    Human PRKCA mRNA encodes the human protein kinase C alpha (PRKCA) protein, a member of Protein kinase C (PKC) family. PRKCA has been reported to play roles in many different cellular processes, such as cell adhesion, cell transformation, cell cycle checkpoint, and cell volume control.
    Human PRKCA mRNA
  • HY-164518
    PF-3837

    		Mps1 Apoptosis Cancer
    PF-3837 is an Mps1 kinase inhibitor with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. PF-3837 interferes with the cell cycle checkpoint by inhibiting Mps1 catalytic activity, reducing genomic stability, thereby inducing cancer cell apoptosis (Apoptosis). PF-3837 can be used in research on breast cancer .
    PF-3837
  • HY-160691
    GW814408X

    		Aurora Kinase Others
    GW814408X is a kinase chemical genome group (KCGS) compound that inhibits the AURKC kinase involved in cell cycle progression, checkpoint regulation, and cell division. GW814408X exhibits cell line-dependent toxicity, e.g., cytotoxic effects on HeLa cells. GW814408X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
    GW814408X
  • HY-125010
    Dicycloplatin

    		DNA/RNA Synthesis Apoptosis Cancer
    Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
    Dicycloplatin
  • HY-E70676
    CDK20/CycT1 Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK20 is a major controller of cell cycle checkpoints, which regulate cell growth and proliferation and perform a role in the development of many malignancies. CDK20 is thought to have Cyclin-dependent activating kinase (CAK) activity for CDK2 when it is complexed with Cyclin H. CDK20/CycT1 Recombinant Human Active Protein Kinase is an ortholog of CDK20 .
    CDK20/CycT1 Recombinant Human Active Protein Kinase
  • HY-P10574
    Phosphorylated CHKtide

    		Checkpoint Kinase (Chk) Cancer
    Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, which is phosphorylated by CHK1/CHK2 in one of the DNA repair pathways. Phosphorylated CHKtide is used in the assays of cell cycle checkpoint kinases 1 and 2 (CHK1/CHK2) and salt-inducible kinases (SIKs) .
    Phosphorylated CHKtide
  • HY-E70675
    CDK20/CycH Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK20 is a major controller of cell cycle checkpoints, which regulate cell growth and proliferation and perform a role in the development of many malignancies. CDK20 is thought to have Cyclin-dependent activating kinase (CAK) activity for CDK2 when it is complexed with Cyclin H. CDK20/CycH Recombinant Human Active Protein Kinase can be used to study the function of CDK20/CycH .
    CDK20/CycH Recombinant Human Active Protein Kinase
  • HY-15882
    GNE-783

    		Endogenous Metabolite Cancer
    GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
    GNE-783
  • HY-164519
    PF-7006

    		Apoptosis Mps1 Mitosis Cancer
    PF-7006 is an Mps1 kinase inhibitor with a Ki value of 0.27 nM and an IC50 value of 2.5 nM. PF-7006 interferes with cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reducing histone H3 levels, and shortening the duration of mitosis, leading to apoptosis in cancer cells. Combined use of PF-7006 with Palbociclib (HY-50767) increases cancer cell tolerance to PF-7006. PF-7006 can be used for breast cancer research .
    PF-7006
  • HY-117102
    ANI-7

    		Aryl Hydrocarbon Receptor Checkpoint Kinase (Chk) Cancer
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
    ANI-7
  • HY-19916A
    Lisavanbulin dihydrochloride

    BAL-101553 dihydrochloride

    		 Microtubule/Tubulin Checkpoint Kinase (Chk) Cancer
    Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin dihydrochloride has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin dihydrochloride is also a spindle assembly checkpoint activator. Lisavanbulin dihydrochloride induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin dihydrochloride can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
    Lisavanbulin dihydrochloride
  • HY-13661
    7-Hydroxystaurosporine

    UCN-01; KRX-0601

    		 Akt PKC CDK Apoptosis Cancer
    7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
    7-Hydroxystaurosporine
  • HY-19916
    Lisavanbulin

    BAL-101553

    		 Microtubule/Tubulin Checkpoint Kinase (Chk) Cancer
    Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator. Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
    Lisavanbulin
  • HY-171785
    CHK1-IN-12

    		Checkpoint Kinase (Chk) Apoptosis Cancer
    CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC50≤10 nM and cellular IC50≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers .
    CHK1-IN-12
  • HY-130841
    Apcin-A

    		APC Ligands for Target Protein for PROTAC Cancer
    Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
    Apcin-A
  • HY-13224A
    AZD4877 hydrochloride

    		Endogenous Metabolite Cancer
    AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
    AZD4877 hydrochloride
  • HY-116190
    CFI-401870

    		Mps1 Cancer
    CFI-401870 is an orally active threonine tyrosine kinase (TKK (Mps1)) inhibitor with an IC50 of 3.1 nM. CFI-401870 exhibits IC50s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer .
    CFI-401870
  • HY-106958
    Talviraline

    HBY 097

    		 HIV Reverse Transcriptase Infection
    Talviraline is a non-nucleoside reverse transcriptase (NNRT) inhibitor that is primarily used to inhibit the replication of human immunodeficiency virus type 1 (HIV-1). Talviraline inhibits the viral replication process by binding to a specific site of HIV-1 reverse transcriptase (RT). Talviraline can be used to study the potential countermeasures and safety of HIV-1 infection .
    Talviraline
  • 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-175236
    SF-9-2

    		PD-1/PD-L1 Apoptosis ERK JNK Cadherin p38 MAPK GSK-3 IFNAR Caspase Bcl-2 Family Cancer
    SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
    SF-9-2

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