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Chk

Chk

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."

Chk related products

Structure Cat No. Product Name CAS No. Product Description
AZD7762 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.
CBP501 Affinity Peptide V54441 CBP501 Affinity Peptide 1351804-17-5 CBP501 Affinity Peptide is a Chk kinase inhibitor that abolishes G2 arrest induced by DNA damaging agents.
CCT-241533 HCl 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.
CCT241533 dihydrochloride 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.
CCT244747 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.
CCT245737 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.
CHIR-124 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.
Chk1-IN-5 V52257 Chk1-IN-5 2120398-39-0 Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor.
Chk1-IN-6 V54449 Chk1-IN-6 2428423-77-0 Chk1-IN-6 is a potent, selective and orally bioavailable CHK1 inhibitor candidate.
Chk2 Inhibitor II (BML-277) 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.
Chktide V54450 Chktide 289652-77-3 Chktide is a substrate of CHK1 and CHK2.
GDC-0575 (ARRY-575, RG7741) 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.
GDC-0575 2HCl 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.
MK-8776 (SCH 900776) 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.
PF-477736 (PF-00477736) 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.
PV-1019 (NSC 744039) 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.
Rabusertib (LY2603618) 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.
SCH900776 S-isomer (MK-8776 S-isomer) 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.
Zn-DPA-maytansinoid conjugate 1 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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