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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
(E/Z)-Chk2-IN-1 V111048 (E/Z)-Chk2-IN-1 693222-51-4 (E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analog-1) (compound 1) is a potent and selective inhibitor of the cell cycle kinase Chk2 with an IC50 value of 8 nM.
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.
BEN-28010 V129990 BEN-28010 3033961-38-2 BEN-28010 is a highly selective, orally effective, blood-brain barrier-crossing CHK1 inhibitor with an IC50 value of 4.0 nM.
CBP-501 acetate V131174 CBP-501 acetate CBP-501 acetate is a cell-permeable calmodulin-binding peptide and a candidate drug for G2 phase blockade. It can inhibit the activity of various Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1, and CHK2, with IC50 values of 0.9 μM, 1.4 μM, 3.4 μM, and 6.5 μM, respectively.
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-11 V131525 CHK1-IN-11 3017958-71-0 CHK1-IN-11 is an orally effective checkpoint kinase 1 (CHK1) inhibitor.
CHK1-IN-12 V131526 CHK1-IN-12 2871056-82-3 CHK1-IN-12 is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with an in vitro enzyme IC50 ≤ 10 nM and a cellular IC50 ≤ 50 nM.
CHK1-IN-13 V131527 CHK1-IN-13 2120398-52-7 CHK1-IN-13 is a checkpoint kinase 1 (Chk1) inhibitor with an IC50 of 10-50 nM.
CHK1-IN-14 V116451 CHK1-IN-14 1803106-00-4 CHK1-IN-14 is a CHK1 inhibitor in its free base form.
CHK1-IN-15 V110208 CHK1-IN-15 CHK1-IN-15 (compound 9a) is an ATP-competitive checkpoint kinase 1 (CHK1) inhibitor with a binding rate of 95% at a concentration of 1.0 µM.
CHK1-IN-4 hydrochloride V99894 CHK1-IN-4 hydrochloride CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (CHK1) inhibitor that effectively inhibits CHK1 phosphorylation in tumor cells.
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.
CHK1-IN-8 V131528 CHK1-IN-8 2871057-47-3 CHK1-IN-8 is a Chk1 inhibitor with an IC50 of <10 nM for human Chk1.
CHK1-IN-9 V88618 CHK1-IN-9 CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 of 0.55 nM.
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