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CAS No.: 1229582-33-5

URMC-099 Catalog No. CSN15761

Synonyms: URMC-099

URMC-099 is an orally bioavailable, brain penetrant inhibitor of Mixed Lineage Kinase 3 (MLK3) with IC50 of 14 nM. It inhibits LPS-induced TNFα release in microglial cells, HIV-1 Tat-induced release of cytokines in human monocytes, and up-regulation of phospho-JNK in Tat-injected brains of mice.

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400-920-2911

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实验方案

技术信息

生物活性

描述Mixed lineage kinase (MLK) belongs to the MAPKKK superfamily and MLK3 is one of the members of the MLK family which regulates the JNK and p38 MAPK signaling cascades to transduce different immune responses. URMC-099 is a blood brain barrier penetrant inhibitor of MLK3 with IC50 value of 14nM. URMC-099 significantly inhibits LPS-induced TNFα release in microglial cells and HIV-1 Tat-induced cytokines release in human monocytes in a dose dependent manner. Tat exposed animals treated with URMC-099 (10mg/kg every twelve hours) showed decreased phosphorylated JNK levels compared with those in untreated models. It also reduced 64.1% and 66.2% of β-amyloidosis load in cortex and hippocampus, respectively, in APP/PS1 mice administered of intraperitoneal URMC-099 injections at 10 mg/kg daily for 3 weeks. URMC-099 also showed anti-migration property in breast cancer cell lines (MDA-MB-231, eGFP8.4 and Hs578t) with IC50 values ranging in 123-231nM, but showed no significant effect on size of breast cancer brain metastases in mouse xenograft model.
作用机制URMC-099 inhibits MLK3 by interacting with MLK3 ATP binding site.
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Goodfellow VS, Loweth CJ, et al. Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48.
[2] Marker DF, Tremblay Me, et al. The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disorders. J Neurosci. 2013 Jun 12;33(24):9998-10010.
[3] Kiyota T, Machhi J, et al. URMC-099 facilitates amyloid-β clearance in a murine model of Alzheimer's disease. J Neuroinflammation. 2018 May 5;15(1):137.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3723 mL
- 11.8614 mL
- 23.7227 mL
- 5 mM
- 0.4745 mL
- 2.3723 mL
- 4.7445 mL
- 10 mM
- 0.2372 mL
- 1.1861 mL
- 2.3723 mL

技术信息

CAS号

1229582-33-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H27N5

运输

蓝冰

分子量

421.54

别名

URMC-099

溶解度

DMSO	71.67 mg/mL (170.0 mM)
Water	insoluble

动物实验配方

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