产品描述:
URMC-099 is an orally bioavailable, brain-penetrant inhibitor of mixed-lineage kinases (MLKs) with IC50 values of 19, 42, 14, and 150 nM for MLK1, MLK2, MLK3, and the related MLK family member DLK, respectively.{19147} It also inhibits LRRK2 activity with an IC50 value of 11 nM.{19147} In vitro, URMC-099 has been shown to reduce inflammatory cytokine production by HIV-1 Tat-exposed microglia and to prevent destruction and phagocytosis of cultured neuronal axons by these cells.{31033} In rodent models of HIV-associated neurocognitive disorders, URMC-099 demonstrates anti-inflammatory and neuroprotective effects.{31033}