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) Agonist
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Checkpoint Kinase (Chk) Activators
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Checkpoint Kinase (Chk) Degraders
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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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(S)-CCT245737
0 ImagesCat. No.: HY-18958ACAS No.: 1489389-23-2Synonyms: (S)-SRA737(S)-CCT245737 ((S)-SRA737) is a potent and selective oral inhibitor of checkpoint kinase 1 (CHK1).
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Phosphorylated CHKtide
0 ImagesCat. No.: HY-P10574Phosphorylated 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).
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Chek1 Mouse Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS02617Chek1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Chek1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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PROTAC FLT3/CHK1 Degrader-1
0 ImagesCat. No.: HY-178858PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
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XL-844
0 ImagesCat. No.: HY-124774CAS No.: 631864-00-1Synonyms: EXEL-9844
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CHK1-IN-12
0 ImagesCat. No.: HY-171785CAS No.: 2871056-82-3CHK1-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.
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Cyproheptadine (Standard)
0 ImagesCyproheptadine (Standard) is the analytical standard of Cyproheptadine (HY-B1622). This product is intended for research and analytical applications. Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine 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 induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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Americanin A
0 ImagesCat. No.: HY-N18301CAS No.: 69506-79-2Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.
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M2I-1 (Standard)
0 ImagesCat. No.: HY-100341RCAS No.: 312271-03-7
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PV1162
0 ImagesCat. No.: HY-164523CAS No.: 1093793-11-3PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy.
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PF 477736 (Standard)
0 ImagesCat. No.: HY-10032RCAS No.: 952021-60-2Synonyms: PF 00477736 (Standard)PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
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Benfluron hydrochloride
0 ImagesCat. No.: HY-106419ACAS No.: 80427-58-3Synonyms: Benflurone hydrochlorideBenfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC50 of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.
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(E/Z)-PV1162
0 ImagesCat. No.: HY-164523ACAS No.: 1346559-65-6
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Prexasertib lactate
0 ImagesCat. No.: HY-18174HCAS No.: 2781996-46-9Synonyms: LY2606368 lactatePrexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity.
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CHK1-IN-4
0 ImagesCat. No.: HY-128766CAS No.: 2120398-41-4CHK1-IN-4 is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 ≤ 1 nM. The IC50 value of CHK1-IN-4 against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 can be used for the research of colon cancer and breast cancer.
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AZD-7762 hydrochloride (Standard)
0 ImagesCat. No.: HY-10992ARCAS No.: 1246094-78-9AZD-7762 hydrochloride (Standard) is the analytical standard of AZD-7762 (hydrochloride) (HY-10992A). This product is intended for research and analytical applications. AZD-7762 hydrochloride is a potent ATP-competitive checkpoint Kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
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GDC-0425 hydrochloride
0 ImagesCat. No.: HY-19926ACAS No.: 1778671-05-8Synonyms: RG-7602 hydrochlorideGDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer.
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Elrelesertib (Standard)
0 ImagesCat. No.: HY-109566RCAS No.: 2089288-03-7Synonyms: AZD1390 (Standard)Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer.
