URMC-099 1229582-33-5

简要描述：URMC-099 1229582-33-5
URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM

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URMC-099 1229582-33-5

产品描述
描述	URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM.
纯度	98%
储存/保存方法	Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性	Ethanol ；6 mg/mL (14.2 mM) DMSO ：75 mg/mL (177.9 mM)
生物活性
靶点	Abl1 ,LRRK2 ,MLK3 ,MLK1 ,VEGFR1/FLT1
In vitro(体外研究)	URMC-099 inhibits LPS-induced TNFα release in microglial cells, and HIV-1 Tat-induced release of cytokines in human monocytes. URMC-099 prevents destruction and phagocytosis of cultured neuronal axons by microglia cells. URMC-099 reduces fMLP-induced chemotaxis of wild-type neutrophil in vitro.
In vivo(体内研究)	In mice, URMC-099 shows excellent pharmacokinetic properties and improved CNS penetration. In vivo, URMC-099 (10 mg/kg i.p.) reduces inflammatory cytokine production, protects neuronal architecture, and alters the morphologic and ultrastructural response of microglia to HIV-1 Tat exposure. URMC099 significantly reduces recruitment of neutrophils into the peritoneum by fMLP in wild-type mice.
参考文献
参考文献	1. Goodfellow VS, et al. J Med Chem. 2013, 56(20), 8032-8048. 2. Marker DF, et al. J Neurosci. 2013, 33(24), 9998-10010.

研究领域
研究领域	CancerOncoproteins/suppressorsOncoproteinsSignal transducers EpigeneticsTranscriptionCancer susceptibilityProto-oncogenes NeuroscienceDevelopment Signal TransductionProtein PhosphorylationTyrosine KinasesOther Drug DiscoverySmall Molecule DrugLead Compound Discovery

URMC-099 1229582-33-5温馨提示：本产品仅作科研实验使用，不支持临床等研究

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