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 (137)
Related Products (137)
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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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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 (PF 00477736) (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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Tubulozole hydrochloride
0 ImagesCat. No.: HY-119169ACAS No.: 83086-73-1Synonyms: R 46846 hydrochlorideTubulozole hydrochloride (R 46846 hydrochloride) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole hydrochloride induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole hydrochloride arrests Mitosis at the metaphase stage. Tubulozole hydrochloride causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole hydrochloride exerts anticancer activity against colon cancer. Tubulozole hydrochloride produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole hydrochloride is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma.
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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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Prexasertib (Standard)
0 ImagesCat. No.: HY-18174RCAS No.: 1234015-52-1Synonyms: LY2606368 (Standard)Prexasertib (Standard) is the analytical standard of Prexasertib (HY-18174). This product is intended for research and analytical applications. Prexasertib (LY2606368) 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 inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib 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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CX-5461 (Standard)
0 ImagesCX-5461 (Standard) is the analytical standard of CX-5461 (HY-13323). This product is intended for research and analytical applications. CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.
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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.
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GDC-0575-d4
0 ImagesCat. No.: HY-112167SSynonyms: ARRY-575-d4; RG7741-d4GDC-0575-d4 (ARRY-575-d4) is the deuterium labeled GDC-0575 (HY-112167). GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
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CHK-IN-1
0 ImagesCat. No.: HY-U00345CAS No.: 1278405-51-8
