CHIR-124 - ≥99%, high purity , CAS No.405168-58-3, Inhibitor of checkpoint kinase 1

Item Number
C125171
Grouped product items
SKUSizeAvailabilityPrice Qty
C125171-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$19.90
C125171-5mg
5mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$49.90
C125171-25mg
25mg
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$159.90
C125171-50mg
50mg
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$259.90
C125171-100mg
100mg
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$419.90

Novel\xa0and potent Chk1 inhibitor

Basic Description

SynonymsNCGC00346626-04 | 4-[(3s)-1-Azabicyclo[2.2.2]oct-3-Ylamino]-3-(1h-Benzimidazol-2-Yl)-6-Chloroquinolin-2(1h)-One | (S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one | BDBM50185219 | 4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsCHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. Chk1 kinase is a critical regulator of both the S and G2/M phase cell cycle checkpoints in response to DNA damage. CHIR-124 has been shown that inhibitors of chk1 can selectively sensit
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of checkpoint kinase 1
NoteRefer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.

Associated Targets(Human)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (6846 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-435 (38290 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-6-chloro-1H-quinolin-2-one
INCHI InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1
InChi Key MOVBBVMDHIRCTG-LJQANCHMSA-N
Canonical SMILES C1CN2CCC1C(C2)NC3=C(C(=O)NC4=C3C=C(C=C4)Cl)C5=NC6=CC=CC=C6N5
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

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
E2420131Certificate of AnalysisFeb 21, 2024 C125171
E2420132Certificate of AnalysisFeb 21, 2024 C125171
E2420133Certificate of AnalysisFeb 21, 2024 C125171
E2420134Certificate of AnalysisFeb 21, 2024 C125171
E2420135Certificate of AnalysisFeb 21, 2024 C125171
E2420136Certificate of AnalysisFeb 21, 2024 C125171
E2420137Certificate of AnalysisFeb 21, 2024 C125171
E2420138Certificate of AnalysisFeb 21, 2024 C125171
E2420139Certificate of AnalysisFeb 21, 2024 C125171
E2420140Certificate of AnalysisFeb 21, 2024 C125171

Chemical and Physical Properties

SolubilityDMSO 7 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Related Documents

References

1. Ni ZJ, Barsanti P, Brammeier N, Diebes A, Poon DJ, Ng S, Pecchi S, Pfister K, Renhowe PA, Ramurthy S et al..  (2006)  4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors..  Bioorg Med Chem Lett,  16  (12): (3121-4).  [PMID:16603354] [10.1021/op500134e]

Solution Calculators