CHIR-124 - Moligand™, 10mM in DMSO , Inhibitor of checkpoint kinase 1, CAS No.405168-58-3, Inhibitor of checkpoint kinase 1

CAS: 405168-58-3 Cat. No.: C407832 Molecular Weight: 419.91 PubChem CID: 135399748

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

CHIR-124 is a novel and potentChk1inhibitor withIC50of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
In vitro

CHIR-124 is a quinolone-based small molecule that is structurally unrelated to other known inhibitors of Chk1. CHIR-124 interacts synergistically with topoisomerase poisons (e.g., Camptothecin or SN-38) in causing growth inhibition in a variety of cancer cell lines, including breast carcinoma (MDA-MB-231 and MDA-MB-435) and colon carcinoma (SW-620 and Colo205), all of which contains the mutant p53 gene. CHIR-124 abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells. The abrogation of the G2-Mcheckpoint and induction of apoptosis by CHIR-124 are enhanced by the loss of p53. CHIR-124 also potently targets other kinases such as PDGFR and Flt3 with IC50 of 6.6 nM and 5.8 nM, respectively.

In vivo

CHIR-124 potentiates the growth inhibitory effects of Irinotecan by abrogating the G₂-M checkpoint and increasing tumor apoptosis in an orthotopic breast cancer xenograft model.
Cell Data

cell lines：

Concentrations：0-2350 nM, dependent on cell types

Incubation Time：48 hours

Powder Purity:≥99%

Specifications

Synonyms

(S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against CDK2/4 and Cdc2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of checkpoint kinase 1

Names and Identifiers

• Isomeric SMILES: C1CN2CCC1[C@@H](C2)NC3=C(C(=O)NC4=C3C=C(C=C4)Cl)C5=NC6=CC=CC=C6N5
• PubChem CID: 135399748
• Molecular Weight: 419.91

Associated Targets(Human)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 (2 Activities)

Discover Target: CHEK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 48 mg/mL (198.08 mM); Ethanol: 48 mg/mL (198.08 mM); Water: Insoluble