Checkpoint Kinase (Chk)
DNA damage checkpoint and the spindle checkpoint are two cell cycle surveillance systems, which guard against genomic instability. The DNA damage checkpoint kinases CHK1 and CHK2 are central to the induction of cell cycle arrest, DNA repair, and apoptosis as elements in the DNA-damage checkpoint. The components of the spindle checkpoint include Mad1, Mad2, Mad3(BubR1), Bub3 and the kinases Bub1, Mph1(Mps1) and Aurora B.
Cells that suffer DNA damage activate the checkpoint kinases CHK1 and CHK2, which signal to initiate repair processes, limit cell-cycle progression and prevent cell replication, until the damaged DNA is repaired.
The spindle checkpoint causes metaphase arrest when kinetochore-microtubules are unattached during mitosis. The SAC consists of ‘sensor’ proteins, such as Mad1, Bub1 and Mps1; a ‘signal transducer’, consisting of the mitotic checkpoint complex, composed of Mad2, Bub3, BubR1 and Cdc20; and an ‘effector’ known as the anaphase promoting complex/cyclosome (APC/C).
Checkpoint Kinase (Chk) Isoform Specific Products
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Checkpoint Kinase (Chk) Inhibitors
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Checkpoint Kinase (Chk) Substrates
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Checkpoint Kinase (Chk) Ligands
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Checkpoint Kinase 1 (Chk1) Proteins
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Checkpoint Kinase 2 (Chk2) Proteins
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Checkpoint Kinase (Chk) Related Products (122)
Related Products (122)
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Recombinant Proteins (6)
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Antibodies (10)
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Checkpoint Kinase (Chk) Isoform Comparison
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Apoptosis inducer 49
0 ImagesCat. No.: HY-178940Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia.
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Theaflavin-3-gallate (Standard)
0 ImagesCat. No.: HY-N0245RCAS No.: 30462-34-1Theaflavin-3-gallate (Standard) is the analytical standard of Theaflavin-3-gallate. This product is intended for research and analytical applications. Theaflavin-3-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3-gallate reacts directly with reduced glutathione (GSH) in a time- and concentration-dependent manner. Theaflavin-3-gallate induces apoptosis and G1 cell cycle arrest in ovarian cancer A2780/CP70 cells through p53-dependent pathways. Theaflavin-3-gallate induces DNA damage through ATM/Chk/p53 pathway.
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MA203
0 ImagesCat. No.: HY-179157MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers.
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CBP501 Affinity Peptide
0 ImagesCat. No.: HY-P4978CAS No.: 1351804-17-5CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research.
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NSC 109555 ditosylate
0 ImagesCat. No.: HY-103366CAS No.: 66748-43-4NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer.
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Zn-DPA-maytansinoid conjugate 1
0 ImagesCat. No.: HY-151559CAS No.: 3034629-04-1Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
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Chk2-IN-1
0 ImagesCat. No.: HY-112477CAS No.: 724708-21-8Synonyms: Hymenialdisine analogue-1Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.
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GDC0575 hydrochloride
0 ImagesCat. No.: HY-112167BCAS No.: 1196504-54-7Synonyms: ARRY-575 hydrochloride; RG7741 hydrochloride
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(E/Z)-Chk2-IN-1
0 ImagesCat. No.: HY-112477ACAS No.: 693222-51-4Synonyms: (E/Z)-Hymenialdisine analogue-1(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
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Chktide
0 ImagesCat. No.: HY-P5961CAS No.: 289652-77-3Chktide is a synthetic peptide substrate applicable for activity assays of Chk1 kinase and cyk/CaMKII. Chktide contains the Ser53 phosphorylation site of Xenopus cyclin B2.
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CCT241533 dihydrochloride
0 ImagesCat. No.: HY-110331CAS No.: 1962925-28-5CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
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PROTAC ATR degrader-3
0 ImagesCat. No.: HY-182016CAS No.: 3126270-11-6PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
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CHK1-IN-9
0 ImagesCat. No.: HY-161383CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).
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Cyproheptadine hydrochloride-d3
0 ImagesCat. No.: HY-W745430Synonyms: Cyproheptadine HCl-d3Cyproheptadine hydrochloride-d3 (Cyproheptadine HCl-d3) is the d3-labeled Cyproheptadine (hydrochloride) (HY-B0366A). Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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CHK1-IN-13
0 ImagesCat. No.: HY-177027CAS No.: 2120398-52-7CHK1-IN-13 (Compound 38) is a checkpoint kinase 1 (Chk1) inhibitor with an IC50 of 10-50 nM. CHK1-IN-13 has anticancer activity, and can be used for the research of cancers, such as breast, ovarian and prostate cancer.
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Multi-kinase-IN-6
0 ImagesCat. No.: HY-156470CAS No.: 3009081-73-3Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
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CHK1-IN-14
0 ImagesCat. No.: HY-177551CAS No.: 1803106-00-4CHK1-IN-14 is a free base form of CHK1 inhibitor. CHK1-IN-14 can be used in research on resistance to chemotherapy and radiotherapy.
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DB07006
0 ImagesCat. No.: HY-160948CAS No.: 622855-60-1DB07006 (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.
