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Chemical Structure| 1300031-52-0 Chemical Structure| 1300031-52-0

Structure of GSK1324726A
CAS No.: 1300031-52-0

Chemical Structure| 1300031-52-0

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GSK1324726A is an inhibitor of BET proteins BRD2, BRD3, BRD4 with IC50 of 41 nM, 31 nM, and 22 nM respectively.

Synonyms: I-BET726

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Product Details of GSK1324726A

CAS No. :1300031-52-0
Formula : C25H23ClN2O3
M.W : 434.91
SMILES Code : O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1
Synonyms :
I-BET726
MDL No. :MFCD28144683
InChI Key :FAWSUKOIROHXAP-NPMXOYFQSA-N
Pubchem ID :52912222

Safety of GSK1324726A

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

Related Pathways of GSK1324726A

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD2, IC50:31 nM

    BRD4, IC50:22 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
SK–N–SH and CHP-212 cells 100 nM or 1 µM 16 hours To analyze the transcriptional changes induced by GSK1324726A in neuroblastoma cell lines using Illumina microarrays. Results showed that GSK1324726A treatment led to significant changes in gene expression, involving apoptosis, signaling, and N-Myc-driven pathways. PMC3751846
CHP-212 cells 250 nM or 1 µM 48 hours To assess the effect of GSK1324726A on the cell cycle of CHP-212 cells. Results showed that GSK1324726A treatment induced G1 phase arrest and increased the sub-G1 fraction at higher concentrations. PMC3751846
Neuroblastoma cell lines 75 nM (gIC50) 6 days To evaluate the growth inhibition and cytotoxic effects of GSK1324726A on neuroblastoma cell lines. Results showed that all tested neuroblastoma cell lines exhibited significant growth inhibition, with most cell lines showing net cell death. PMC3751846

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Human neuroblastoma xenograft models Oral 5 mg/kg or 15 mg/kg Once daily for 14 days (SK–N-AS model) or 42 days (CHP-212 model) To evaluate the inhibitory effect of GSK1324726A on neuroblastoma tumor growth in vivo. Results showed that GSK1324726A treatment significantly inhibited tumor growth and downregulated MYCN and BCL2 expression. PMC3751846

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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