URMC-099 是一种具有优异的血脑屏障穿透性的，可口服的混合谱系激酶 3 抑制剂，IC50为14 nM。

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

URMC-099（10 mg/kg, i.p. ）可减少体内炎性细胞因子产生,保护神经元结构,并改变小胶质细胞对HIV-1 Tat暴露下的形态和超微响应.URMC-099在小鼠体内,表现出良好的药代动力学性能和改善的CNS渗透性.URMC099明显减少野生型小鼠体内中性粒细胞通过fMLP进入腹膜.

URMC-099可降低体外实验中fMLP诱导的野生型嗜中性粒细胞的趋药性。URMC-099还对小胶质细胞中脂多糖诱导的TNFα释放,以及人单核细胞中HIV-1 Tat诱导的细胞因子释放有抑制作用。 URMC-099防止培养的神经轴突被小胶质细胞破坏和吞噬。

HDAC IC50 Profiling: The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company's standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds.

1229582-33-5

C27H27N5

421.548

Ethanol:6 mg/mL (14.2 mM)
H2O:<1 mgml
DMSO:75 mg/mL (177.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years