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.
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- Fòrmula: C33H38N4O3
- Peso molecular:538.68
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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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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Peso molecular 538.68
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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