Product IntroductionBioactivity英文名:
URMC-099描述: 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。
激酶实验: 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.
体外活性: 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.
体内活性: 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。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 6 mg/mL (14.2 mM)
DMSO : 75 mg/mL (177.9 mM)
关键字:
inhibit |
MLKs |
Autophagy |
URMC099 |
URMC 099 |
Inhibitor |
Mixed Lineage Kinase |
URMC-099相关产品:
Thiazovivin |
Fasudil hydrochloride |
Chroman 1 |
CAY10746 |
GSK-25 |
ROCK-IN-2 |
Tofacitinib |
Hydroxyfasudil Hydrochloride |
Verosudil |
Cucurbitacin A相关库:
Anti-Neurodegenerative Disease Compound Library |
Glycometabolism Compound Library |
Membrane Protein-targeted Compound Library |
Bioactive Compounds Library Max |
Inhibitor Library |
Kinase Inhibitor Library |
Tyrosine Kinase Inhibitor Library |
Apoptosis Compound Library |
DNA Damage & Repair Compound Library |
TGF-beta/Smad Compound Library