CHIR-124 - CAS 405168-58-3
Catalog number: 405168-58-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
Checkpoint Kinase (Chk)
Description:
CHIR-124 is a quinolone-based small molecule Chk1 inhibitor, that is structurally unrelated to other known inhibitors of Chk1. It potently and selectively inhibits Chk1 in vitro (IC(50) = 0.0003 micromol/L). CHIR-124 interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines as determined by isobologram or response surface analysis. CHIR-124 is a novel and potent Chk1 inhibitor with promising antitumor activities when used in combination with topoisomerase I poisons.
Publictions citing BOC Sciences Products
  • >> More
Purity:
0.98
Synonyms:
CHIR-124
MSDS:
Inquire
1.Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints.
Tao Y1, Leteur C, Yang C, Zhang P, Castedo M, Pierré A, Golsteyn RM, Bourhis J, Kroemer G, Deutsch E. Cell Cycle. 2009 Apr 15;8(8):1196-205. Epub 2009 Apr 16.
Checkpoint kinase-1 (CHK1) is a key regulator of the DNA damage-elicited G(2)-M checkpoints. The aim of the present study was to investigate the effects of a selective CHK1 inhibitor, Chir124, on cell survival and cell cycle progression following ionizing radiation (IR). Treatment with Chir-124 resulted in reduced clonogenic survival and abrogated the IR-induced G(2)-M arrest in a panel of isogenic HCT116 cell lines after IR. This radiosensitizing effect was relatively similar between p53(-/-) and p53-sufficient wild type (WT) HCT116 cells. However, the number of mitotic cells (as measured by assessing the phosphorylation of mitotic proteins) increased dramatically in p53(-/-) HCT116 cells after concomitant Chir-124 exposure, compared to IR alone, while no such effect was observed in p53-sufficient WT HCT116 cells. In p53(-/-) cells, Chir-124 treatment induced a marked accumulation of polyploid cells that were characterized by micronucleation or multinucleation.
2.CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo.
Tse AN1, Rendahl KG, Sheikh T, Cheema H, Aardalen K, Embry M, Ma S, Moler EJ, Ni ZJ, Lopes de Menezes DE, Hibner B, Gesner TG, Schwartz GK. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602.
PURPOSE: Chk1 kinase is a critical regulator of both S and G(2)-M phase cell cycle checkpoints in response to DNA damage. This study aimed to evaluate the biochemical, cellular, and antitumor effects of a novel Chk1 inhibitor, CHIR124.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Checkpoint Kinase (Chk) Products


CCT245737
(CAS: 1489389-23-2)

CCT245737, a nitrogen heterocycle compound, has been found to be a CHK1 inhibitor that could probable be effective in antineoplastic studies. It is still under ...

CAS 860352-01-8 AZD-7762

AZD-7762
(CAS: 860352-01-8)

AZD-7762 is a synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, whic...

CAS 952021-60-2 PF-477736

PF-477736
(CAS: 952021-60-2)

PF-477736 is a proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity. Chk1 inhibitor PF-477736 inhibits...

CAS 891494-63-6 SCH900776

SCH900776
(CAS: 891494-63-6)

SCH900776, also known as MK-8776. is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activit...

CAS 1234015-55-4 Prexasertib mesylate

Prexasertib mesylate
(CAS: 1234015-55-4)

Prexasertib, also known as LY2606368, is an ATP-competitive CHK1 inhibitor (Ki= 0.9 nmol/L), with minor activity against CHK2 and RSK with IC50= 8 nM and 9 nM r...

GDC-0425
(CAS: 1200129-48-1)

This active molecular is an selective Checkpoint kinase 1 (Chk1) inhibitors and it enhances gemcitabine efficacy in tumor xenograft models. GDC-0425 was safe an...

CAS 1262849-73-9 CCT241533

CCT241533
(CAS: 1262849-73-9)

CCT241533, a Chk2 inhibitor, has been found to improve the effect of genotoxic cancer therapies. IC50: 3 nM.

CCT241533 (hydrochloride)
(CAS: 1431697-96-9)

CCT241533 (hydrochloride) is the hydrochloride salt form of CCT241533. As a potent Chk2 inhibitor, CCT241533 blocked CHK2 activity in human tumor cell lines in ...

CAS 911222-45-2 LY2603618

LY2603618
(CAS: 911222-45-2)

LY2603618 is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to ente...

LY2606368 dihydrochloride
(CAS: 1234015-54-3)

The dihydrochloride salt form of LY2606368 which also known as prexasertib, is an inhibitor of checkpoint kinase 1 and has potential effect in antineoplastic. I...

CAS 405168-58-3 CHIR-124

CHIR-124
(CAS: 405168-58-3)

CHIR-124 is a quinolone-based small molecule Chk1 inhibitor, that is structurally unrelated to other known inhibitors of Chk1. It potently and selectively inhib...

SCH900776 S-isomer
(CAS: 891494-64-7)

SCH900776 S-isomer is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1. It can be used a...

CAS 516480-79-8 BML-277

BML-277
(CAS: 516480-79-8)

BML-277 is a selective APT-competitive inhibitor of the DNA damage response signaling enzyme CHK2 ( IC50 =15 nM).

CAS 1278405-51-8 Thieno[2,3-d]pyridazine-7-carboxamide, 2-(3-fluorophenyl)-4-[(3S)-3-piperidinylamino]-, hydrochloride

Thieno[2,3-d]pyridazine-7-carboxamide, 2
(CAS: 1278405-51-8)

An inhibitor of CHK1 and CHK2

CAS 1234015-52-1 LY2606368

LY2606368
(CAS: 1234015-52-1)

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

Chemical Structure

CAS 405168-58-3 CHIR-124

Quick Inquiry

Verification code

Featured Items