GSK789
GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases.
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- CAS No.: 2540591-06-6
- Formule: C26H33N5O3
- Masse moléculaire:463.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
390 nM
Compound: 42, GSK789, Single enantiomer
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Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay
Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay
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[PMID: 32691589] |
| MV4-11 | IC50 |
124.6 nM
Compound: 42, GSK789, Single enantiomer
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Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay
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[PMID: 32691589] |
| THP-1 | IC50 |
158 nM
Compound: 42, GSK789, Single enantiomer
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Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay
Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay
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[PMID: 32691589] |
GSK789 (Compound 42) binds efficiently to BRD2 BD1, BRD3 BD1, BRD4 BD1 and BRDT BD1 (pKd = 7.7-8.4)[1].
GSK789 potently inhibits BRD4 BD1 (pIC50 = 7.5) and inhibits BRD4 BD2 (pIC50 = 4.5) in TR-FRET assays[1].
GSK789 (0.001-100 μM; 3 days) potently inhibits the growth of MV-4-11, HL60 and THP-1 leukemia cell lines, with IC50 values of 124.6 nM, 390.0 nM and 158.0 nM, respectively; complete inhibition is achieved at the concentration with the weakest binding affinity to the BET BD2 domain[1].
GSK789 potently inhibits the production of LPS (HY-D1056)-stimulated MCP-1 (IC50 = 0.67 μM), TNFα (IC50 = 0.87 μM), and IL-6 (IC50 = 3.55 μM) in human whole blood[1].
GSK789 (0.3-10 μM) exhibits a phenotypic fingerprint unique to BD1-selective BET inhibitors in the BioMAP Diversity PLUS platform, and exerts antiproliferative, anti-inflammatory and immunomodulatory effects in human primary cell assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human leukemia cell lines (MV-4-11, HL60, THP-1)
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:3 days
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Result:Inhibited cell growth with an IC50 of 124.6 nM in MV-4-11 cells.
Inhibited cell growth with an IC50 of 390.0 nM in HL60 cells.
Inhibited cell growth with an IC50 of 158.0 nM in THP-1 cells.
Achieved full inhibition at concentrations where BD2 engagement was minimal.
Chemical Information
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CAS No. 2540591-06-6
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Masse moléculaire 463.57
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Formule C26H33N5O3
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SMILES
O=C([C@@H]1CN(C)CC[C@H]1NC2=C3NC(C(C)=CC3=C(C4=CC=CO4)C=N2)=O)NC5CCCCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK789 Related Classifications
HY-138623 Related Classifications
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