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Chemical Structure| 2474876-09-8 Chemical Structure| 2474876-09-8

Structure of GSK046
CAS No.: 2474876-09-8

Chemical Structure| 2474876-09-8

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GSK046 is a BET protein BD2 bromodomain inhibitor that effectively regulates the immune system. It has significant application prospects in immune regulation and cancer research.

Synonyms: iBET-BD2

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Product Details of GSK046

CAS No. :2474876-09-8
Formula : C23H27FN2O4
M.W : 414.47
SMILES Code : C[C@@H](C1=CC=CC=C1)OC2=C(C(F)=CC(C(N[C@H]3CC[C@@H](CC3)O)=O)=C2)NC(C)=O
Synonyms :
iBET-BD2
MDL No. :MFCD32858297

Safety of GSK046

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of GSK046

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD3BD2, IC50:98 nM

    BRD4BD2, IC50:214 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human β-cell line EndoC-βH1 1 μM 24 or 48 hours To evaluate the protective effects of GSK046 on inflammation-induced gene expression in EndoC-βH1 cells. Results showed that GSK046 partially reduced pro-inflammatory gene expression but did not prevent apoptosis. iScience. 2022 Oct 17;25(11):105376
Human islet cells 1 μM 48 hours To evaluate the protective effects of GSK046 on inflammation-induced gene expression in human islet cells. Results showed that GSK046 reduced pro-inflammatory gene expression but did not prevent apoptosis. iScience. 2022 Oct 17;25(11):105376

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

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
 

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