2. Epigenetics Apoptosis Immunology/Inflammation
  3. Epigenetic Reader Domain TNF Receptor Interleukin Related
  4. 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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GSK789

GSK789 Chemical Structure

CAS No. : 2540591-06-6

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GSK789 Related Antibodies

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
390 nM
Compound: 42, GSK789, Single enantiomer
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
[PMID: 32691589]
MV4-11 IC50
124.6 nM
Compound: 42, GSK789, Single enantiomer
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
[PMID: 32691589]
THP-1 IC50
158 nM
Compound: 42, GSK789, Single enantiomer
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
[PMID: 32691589]
In Vitro

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.

GSK789 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human leukemia cell lines (MV-4-11, HL60, THP-1)
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 3 days
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.
Molecular Weight

463.57

Formula

C26H33N5O3
CAS No.
SMILES

O=C([C@@H]1CN(C)CC[C@H]1NC2=C3NC(C(C)=CC3=C(C4=CC=CO4)C=N2)=O)NC5CCCCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSK789 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK7892540591-06-6GSK 789GSK-789Epigenetic Reader DomainTNF ReceptorInterleukin RelatedTumor Necrosis Factor ReceptorTNFRILBET family proteinsBRDT BD1HL60THP-1BRD4 BD1BET BD2 domainsBRD3 BD1MCP-1MV-4-11BRD2 BD1leukemiainflammatoryimmune diseasesInhibitorinhibitorinhibit

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