Two cell cycle surveillance systems, the DNA damage checkpoint and the spindle checkpoint, protect against genomic instability. The DNA-damage checkpoint is made up of three components: DNA repair, apoptosis, and the DNA damage checkpoint kinases CHK1 and CHK2. Mad1, Mad2, Mad3(BubR1), Bub3, and the kinases Bub1, Mph1(Mps1), and Aurora B are parts of the spindle checkpoint.
When cells experience DNA damage, the checkpoint kinases CHK1 and CHK2 become active. These kinases send signals to start DNA repair procedures, regulate cell cycle progression, and stop cell replication until the damaged DNA is repaired.
When kinetochore-microtubules separate during mitosis, the spindle checkpoint causes metaphase arrest. The mitotic checkpoint complex, which is made up of Mad2, Bub3, BubR1, and Cdc20, serves as the mitotic checkpoint complex's "signal transducer" in the SAC. The anaphase promoting complex/cyclosome (APC/C) serves as the SAC's "effector."
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V1582 | AZD7762 | 860352-01-8 | AZD7762 (AZD-7762; AZD 7762) is a selective and ATP-competitive inhibitor of Chk1 (checkpoint kinases) with potential anticancer activity. |
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V54441 | CBP501 Affinity Peptide | 1351804-17-5 | CBP501 Affinity Peptide is a Chk kinase inhibitor that abolishes G2 arrest induced by DNA damaging agents. |
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V5293 | CCT-241533 HCl | 1431697-96-9 | CCT241533 HCl, the dihydrochloride salt of CCT-241533, is a novel, potent and selective CHK2 inhibitor with anticancer activity. |
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V52290 | CCT241533 dihydrochloride | 1962925-28-5 | CCT241533 diHCl is a potent and specific CHK2 inhibitor (antagonist) with IC50 and Ki of 3 nM and 1.16 nM respectively. |
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V17742 | CCT244747 | 1404095-34-6 | CCT-244747 is a novel, potent, highly selective and orally bioavailable ATP-competitive CHK1 inhibitor (IC50= 7.7 nM) with potential anticancer activity. |
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V2732 | CCT245737 | 1489389-18-5 | CCT245737 (CCT-245737) is a novel, potent, orally bioavailable and selective ATP-competitive inhibitor of CHK1 (checkpoint kinase 1) with anticancer activity. |
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V1585 | CHIR-124 | 405168-58-3 | CHIR-124 (CHIR124; CHIR 124) is a novel, potent and selective quinolone-based small molecule Chk1 (Checkpoint kinase1) inhibitor with potential anticancer activity. |
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V52257 | Chk1-IN-5 | 2120398-39-0 | Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. |
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V54449 | Chk1-IN-6 | 2428423-77-0 | Chk1-IN-6 is a potent, selective and orally bioavailable CHK1 inhibitor candidate. |
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V3119 | Chk2 Inhibitor II (BML-277) | 516480-79-8 | Chk2 Inhibitor II (also known as BML-277) is an ATP-competitive inhibitor of Chk2 (checkpoint kinase 2) with an IC50 of 15 nM. |
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V54450 | Chktide | 289652-77-3 | Chktide is a substrate of CHK1 and CHK2. |
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V3690 | GDC-0575 (ARRY-575, RG7741) | 1196541-47-5 | Chk2 Inhibitor II (also known as BML-277) is an ATP-competitive inhibitor of Chk2 (checkpoint kinase 2) with an IC50 of 15 nM. |
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V3691 | GDC-0575 2HCl | 1657014-42-0 | GDC-0575 (also called ARRY-575, RG7741) is a novel, potent and selective inhibitor of CHK1 (Check point kinases) which specifically binds to and inhibits CHK1 with an IC50 of 1.2 nM. |
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V1584 | MK-8776 (SCH 900776) | 891494-63-6 | MK-8776 (also known as SCH900776;MK8776;SCH-900776;MK 8776) is a novel, highly potent and selective Chk1 (cell cycle checkpoint kinase 1) inhibitor with potential antineoplastic, radiosensitization and chemosensitization activities. |
|
V1586 | PF-477736 (PF-00477736) | 952021-60-2 | PF-477736 (also known as PF-736; PF-00477736; PF477736) is a novel, selective, potent and ATP-competitive Chk1 inhibitor with potential antitumor activity. |
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V39684 | PV-1019 (NSC 744039) | 1093793-05-5 | PV-1019 (NSC 744039) is a potent and specific Chk2 inhibitor (antagonist) with IC50 of 24 nM. |
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V1583 | Rabusertib (LY2603618) | 911222-45-2 | Rabusertib (also known as IC-83;LY-2603618; LY 2603618;IC83) is a novel, potent and selective Chk1 (cell cycle checkpoint kinase 2) inhibitor with potential antitumor activity. |
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V28897 | SCH900776 S-isomer (MK-8776 S-isomer) | 891494-64-7 | SCH900776 S-isomer is the S-isomer of SCH900776 (MK-8776), whichis a novel, highly potent and selective Chk1 (cell cycle checkpoint kinase 1) inhibitor with IC50 of 3 nM in a cell-free assay. |
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V51109 | Zn-DPA-maytansinoid conjugate 1 | Zn-DPA-maytansinoid conjugate 1 is a maytansinoid conjugate based on small molecules that targets immune checkpoint. |
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