2. Epigenetics
  3. Epigenetic Reader Domain
  4. GSK761

GSK761 

Cat. No.: HY-148591
Handling Instructions

GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206+ regulatory macrophages by inhibiting SP140.

For research use only. We do not sell to patients.

GSK761 Chemical Structure

GSK761 Chemical Structure

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Description

GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206+ regulatory macrophages by inhibiting SP140[1].

IC50 & Target

IC50: 77.79 nM (Speckled 140 kDa, SP140)[1]
In Vitro

GSK761 combines with SP140 in HuT78 cells and HEK293 cells transfected with Halo-tagged SP140[1].
GSK761 (0.01-1.11 µM; 1 h) reduces the inflammatory activation and down-regulates the expression of TNF, IL-6, IL-12p70, IL-1β, IL-8, IL-10 pro-inflammatory cytokines in M1 polarized macrophages[1].
GSK761 (0.04 µM; 4 h) significantly decreases the expression of TNF, IL6 and IL10 in CD14+ mucosal macrophages[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

646.82

Formula

C40H46N4O4
SMILES

CN1C2=CC=C(C=C2N=C1C3=CC=C(C=C3)C(NC4=CC(CCOC(C)(C)C)=CC=C4)=O)C(NC5=CC(CCOC(C)(C)C)=CC=C5)=O
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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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.

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Keywords:

GSK761GSK 761GSK-761Epigenetic Reader DomainHuT78HEK293MacrophagesInhibitorinhibitorinhibit

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