GSK761

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].

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gsk761.html

Concentration

10mM

Purity

99.42

Solubility

DMSO : 125 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C40H46N4O4

Molecular Weight

646.82

References & Citations

[1]Ghiboub M, et al. Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140. BMC Biol. 2022 Aug 19;20 (1) :182.