Welcome to Raystarbio!Focus On Forefront Bioactive Compounds.
Find Your Distributors

Select Your Country or Region

$ USD

You are here:Home-Inhibitors & Agonists-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)

Request The Product List ofCheckpoint Kinase (Chk) Checkpoint Kinase (Chk)

    Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability.

图。1。

    Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

Cat. No. Product Name CAS No. Information
GY03968

SB218078

135897-06-2

A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM; less potently inhibits Cdc2 and PKC (IC50=250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 uM; enhances the cytotoxicity of DNA-damaging agents.

GY02620

CCT-245737

1489389-18-5

A highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM; weak inhibition on Chk2 (IC50=2440 nM); inhibits genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) both in vitro and in human tumor xenografts; showes significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma; orally active.

GY02560

CCT241533 hydrochloride

1431697-96-9

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation.

GY02503

CCT-244747

1404095-34-6

A novel, potent, highly selective, orally active, ATP competitive CHK1 inhibitor with biochemical IC50 of 8 nM; displays 75-fold selectivity against FLT3 and >1,000-fold selectivity against CHK2 and CDK1; inhibits cellular CHK1 activity (IC50=29-170nM), significantly enhances the cytotoxicity of several anticancer drugs and abrogates drug-induced S and G2 arrest in multiple tumor cell lines; enhances antitumor activity of gemcitabine and irinotecan in vivo.

GY07052

MU 380

2109805-78-7

MU 380 is a novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2; sensitizes a variety of tumor cell lines to hydroxyurea or gemcitabine up to 10 times; shows extended inhibitory effects in cells, and unlike SCH900776, does not undergo in vivo N-dealkylation to the significantly less selective metabolite; causes higher accumulation of DNA damage in tumor cells and subsequent enhanced cell death, and is more efficacious in the A2780 xenograft mouse model.

GY06980

Debromohymenialdisine

75593-17-8

Debromohymenialdisine is a marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively; also inhibits MAP kinase kinase 1 (IC50=881 nM), GSK3β (IC50=1.39 uM), and CDK5/p25 (IC50=9.12 uM), does not significantly affect ATM and ATR; blocks G2 arrest in cancer cells.

GY06979

PD-321852

622856-21-7

PD-321852 is a potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM; potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines; inhibits gemcitabine-induced Rad51 focus formation, and depletes RAD51 proteins in pancreatic cancer cells.

GY05347

GDC-0575

1196541-47-5

GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM; enhances the killing of primary AML cells ex vivo by inducing apoptosis combined with AraC, blocks the activation of CHK1 induced by AraC via decrease in the level of Tyr15-phosphorylated CDK2 at 100 nM in AML cells.

GY02328

CCT241533

1262849-73-9

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM; shows good selectivity for CHK2 against CHK1 (IC50=180 nM) and a wider panel of kinases and with promising in vitro ADMET properties; inhibits CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation.

GY02281

Prexasertib dihydrochloride

1234015-54-3

A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
© Copyright 2020 RayStarBio. All Rights Reserved. Products are only for research use