For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I041417 |
| Synonyms | 1-methyl-N-[3-[2-[(2-methylpropan-2-yl)oxy]ethyl]phenyl]-2-[4-[[3-[2-[(2-methylpropan-2-yl)oxy]ethyl]phenyl]carbamoyl]phenyl]benzimidazole-5-carboxamide |
| Molecular Formula | C40H46N4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C40H46N4O4/c1-39(2,3)47-22-20-27-10-8-12-32(24-27)41-37(45)30-16-14-29(15-17-30)36-43-34-26-31(18-19-35(34)44(36)7)38(46)42-33-13-9-11-28(25-33)21-23-48-40(4,5)6/h8-19,24-26H,20-23H2,1-7H3,(H,41,45)(H,42,46) |
| InChIKey | DAHVZGAYZACXOD-UHFFFAOYSA-N |
| SMILES | CC(C)(C)OCCC1=CC(=CC=C1)NC(=O)C2=CC=C(C=C2)C3=NC4=C(N3C)C=CC(=C4)C(=O)NC5=CC=CC(=C5)CCOC(C)(C)C |
| Reference | [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. |
