IC50: 77.79 nM (Speckled 140 kDa, SP140)[1]
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 在经 halo-tag SP140 转染的 HuT78 细胞和 HEK293 细胞中与 SP140 结合[1]。
GSK761 (0.01-1.11 µM；1 h) 降低了 M1 极化巨噬细胞中的炎症激活，下调了 TNF、IL-6、IL-12p70、IL-1β、IL-8、IL-10 促炎细胞因子的表达[1]。
GSK761 (0.04 µM；4 h) 显著减少了 CD14+ 粘膜巨噬细胞中 TNF、IL6 和 IL10 的表达[1]。
[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.