GSK785
GSK785 is a BRD2/4-selective, BRD3-sparing bivalent BET inhibitor. GSK785 inhibits production of the MCP1 cytokine in human whole blood. GSK785 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Formula: C33H38N4O3
- Molecular Weight:538.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD2 |
BRD4 |
BET |
GSK785 (Compound 9h) (Titrated 1:3 from 1 mM stock in 100% DMSO; 18-24 h) inhibits BRD2, BRD3, and BRD4 in HEK 293 WT cells with pIC50 values of 7.9, 6.9, and 8.5, respectively, showing BRD2/4 selectivity and BRD3 sparing[1].
GSK785 (Titrated 1:3 from 1 mM stock in 100% DMSO; 4 h) binds bivalently to BRD4 in HEK 293 WT cells with a pIC50 of 7.9 in the BRD4 Biosensor assay[1].
GSK785 (1.6 nM-5 μM; 2 h) stabilizes BRD2, BRD3, and BRD4 in HuT 78 cells with pEC50 values of 8.1, 6.0, and 7.0, respectively, confirming BRD2/4 selectivity and BRD3 sparing[1].
GSK785 inhibits production of the MCP1 cytokine in human whole blood with an pIC50 of 7.4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 538.68
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Formula C33H38N4O3
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SMILES
C[C@@H]1C2=CC=C(C=C2C=CN(C1=O)C)CN3CCC4(CC3)CN(C(C5=CC=C6[C@H](C(N(C=CC6=C5)C)=O)C)=O)C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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