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Chemical Structure| 405168-58-3 Chemical Structure| 405168-58-3

Structure of CHIR-124
CAS No.: 405168-58-3

Chemical Structure| 405168-58-3

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

Synonyms: CHIR-124

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Product Details of CHIR-124

CAS No. :405168-58-3
Formula : C23H22ClN5O
M.W : 419.91
SMILES Code : O=C1NC2=C(C=C(Cl)C=C2)C(N[C@@H]3CN4CCC3CC4)=C1C5=NC6=CC=CC=C6N5
Synonyms :
CHIR-124
MDL No. :MFCD14636453

Safety of CHIR-124

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of CHIR-124

RTK

Isoform Comparison

Biological Activity

Target
  • Chk1

    Chk1, IC50:0.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human foreskin fibroblast (HFS) 2 μM 72 hours CHIR-124 sensitized normal cells (HFS) to HDACi-induced cell death and increased HDACi-induced cell death in A549 cells. PMC3241758
Human prostate cancer cells (LNCaP) 2 μM 72 hours CHIR-124 did not significantly increase HDACi-induced cell death in LNCaP cells. PMC3241758
Human lung adenocarcinoma cells (A549) 2 μM 72 hours CHIR-124 increased HDACi-induced cell death in A549 cells. PMC3241758
MDA-MB-231 0.05 μM 72 hours CHIR-124 was able to downregulate BRCA1 protein levels and synergized with olaparib, significantly reducing the proliferation of breast cancer cells. PMC11238136
HEK293T 1 μM 24 hours CHIR-124 showed downregulation of BRCA1 protein levels in HEK293T cells. PMC11238136
HeLa cervical cancer cells 500 nM 48 hours Co-treatment of CHIR-124 with [Ru(dppz)2(PIP)]2+ significantly reduced cell viability in HeLa cells, indicating synergistic induction of apoptosis. PMC4997316
hSAEC1-KT human epithelial cells 500 nM 48 hours Co-treatment of CHIR-124 with [Ru(dppz)2(PIP)]2+ did not show significant impact on hSAEC1-KT cells. PMC4997316
Kasumi-1 cells 200 nM 2 hours CHIR-124, as a CHK1 inhibitor, reduced the ZGDHu-1-induced G2/M phase cell cycle arrest, with the proportion of cells in the G2/M phase decreasing from 40.1±1.4% to 8.6±1.2%. PMC4368067
Capan-2 cells 2 x 10^-8 M 16 hours To evaluate the synergistic cytotoxic effect of CHIR-124 in combination with gemcitabine on Capan-2 spheroids. Results showed that CHIR-124 enhanced gemcitabine-induced DNA damage and apoptosis. PMC3280152

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice Chk1fl/fl Vav-CreERT2 mice oral gavage 1 mg/kg CuET Once every 2 days for 9 weeks To evaluate the role of CHK1 in adult hematopoietic system, results showed that CHK1 deletion led to cell loss, and in vivo experiments, cells retaining CHK1 expression were selectively maintained. PMC6680171

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.91mL

2.38mL

1.19mL

23.81mL

4.76mL

2.38mL

References

 

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