GW2580

GW2580 is a **selective and orally bioavailable small molecule inhibitor** of the tyrosine kinase activity of the **colony-stimulating-factor-1 receptor (CSF-1R, also known as cFMS)**. It binds to CSF-1R (IC50 ~30 nM) and locks the kinase in an inactive conformation. GW2580 is highly selective, with marked inactivity against a panel of more than 25 other kinases. Its primary mechanism is the inhibition of monocyte and microglial proliferation by blocking CSF-1 signaling pathways, which results in reduced macrophage accumulation, suppressed myeloid-derived suppressor cell expansion, and modification of neuroinflammatory responses. Preclinical studies have demonstrated efficacy in animal models of neuroinflammatory and neurodegenerative diseases, including multiple sclerosis, Alzheimer’s disease, amyotrophic lateral sclerosis, and prion disease. GW2580 does not ablate microglia but reduces their proliferation and modulates their transcriptomic and morphological state. Developed primarily as a pharmacological research tool, not a marketed therapeutic.

Other names

5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine