lx3

LX-3 is a selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway, which de-represses a subset of endogenous genes repressed by DNA methylation.

BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).1 It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 μM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro. |1. Archambault, A.-S., Turcotte, C., Martin, C., et al. Comparison of eight 15-lipoxygenase (LO) inhibitors on the biosynthesis of 15-LO metabolites by human neutrophils and eosinophils. PLoS One 13(8), e0202424 (2018).

GLX351322 抑制 NADPH 氧化酶 4 (Nox4) 。在 NOX4 过表达的细胞中，抑制过氧化氢的产生，IC50值为 5 μM。

Pexidartinib (PLX-3397) 是一种 CSF-1R 和 c-Kit 的抑制剂 (IC50=20 10 nM)，具有选择性、ATP 竞争性和口服活性。Pexidartinib 具有抗肿瘤活性，可以诱导细胞凋亡。

RLX-33 是一种有效的、选择性的、能够透过血脑屏障的松弛素家族肽 3 (RXFP3) 拮抗剂，也能够阻断松弛素 3 (relaxin 3) 诱导的 ERK1 2 磷酸化。RLX-33 作用于 RXFP3、ERK1 和 ERK2 磷酸化的 IC50 分别为 2.36 μM、7.82 μM 和 13.86 μM。RLX-33 可以阻断 RXFP3 选择性激动剂 R3 I5 诱导的大鼠食物摄取增加。RLX-33 能够用于研究代谢综合征。

PLX-3618 是一款通过促进 BRD4 的多泛素化进而实现其蛋白酶体降解的单价直接降解剂，具体是通过募集 E3 连接酶底物受体 DCAF11 来执行此功能，DC50 为 12.2 nM。该化合物有效抑制多种癌细胞增殖，并在小鼠模型中显示出抗 AML (acute myeloid leukemia) 肿瘤活性，能够诱导 AML 细胞的凋亡 (apoptosis)。