EHT 1864

EHT 1864用途

EHT 1864是Rac1信号转导抑制剂,能调节_gamma_-分泌酶介导的APP。

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EHT 1864作用

EHT 1864是Rac1信号传导的小分子抑制剂;调节γ-分泌酶介导的APP加工。体外Rac1抑制剂：EHT1864阻断Aβ40和Aβ42的产生但不影响sAPPα水平并且不抑制γ-分泌酶。相反，EHT 1864调节γ-分泌酶水平的APP加工以防止Aβ40和Aβ42的产生。这种效应不是由γ-分泌酶活性的直接抑制引起的，并且对APP裂解是特异性的，因为EHT 1864不影响Notch裂解。 EHT 1864特异性抑制Rac1依赖性血小板衍生生长因子诱导的片状伪足形成。此外，我们用重组Rac蛋白进行的生化分析发现EHT 1864具有高亲和力结合Rac1，以及相关的Rac1b，Rac2和Rac3同种型，这种关联促进结合核苷酸的缺失，抑制鸟嘌呤核苷酸结合和Tiam1 Rac鸟嘌呤核苷酸交换因子刺激体外交换因子活性。体内：EHT1864显着降低豚鼠脑中的Aβ40和Aβ42水平，其阈值与延迟斑块积聚和/或清除脑中现有斑块相容。

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EHT 1864名称

[ CAS 号 ]:
754240-09-0

[ 中文名 ]:
EHT 1864

[ 英文名 ]:
EHT 1864

[英文别名 ]:

eht 1864
EHT-1864

EHT 1864生物活性

[ 描述 ]:

EHT 1864是Rac1信号转导抑制剂,能调节_gamma_-分泌酶介导的APP。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 拉斯

研究领域 >> 神经疾病

[参考文献]

[1]. Desire L, et al. RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo. J Biol Chem. 2005 Nov 11;280(45):37516-25.

[2]. Shutes A, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. J Biol Chem. 2007 Dec 7;282(49):35666-78.

[3]. Onesto C, et al. Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 2008;439:111-29.

[相关活性小分子]

ARS-853 | ARS-1620 | NSC 23766三盐酸盐 | ML141 | 2-[[(2E,6E)-3,7,11-三甲基-2,6,10-十二烷三烯-1-基]硫代]苯甲酸 | 泛RAS-IN-1 | 盐酸罗红 | CASIN | N4-(9-乙基-9H-咔唑-3-基)-N2-[3-(4-吗啉基)丙基]-2,4-嘧啶二胺 | 图1A-116 | CCG-1423 | K-Ras(G12C) inhibitor 12 | ZCL278 | Y16 | BQU57

EHT 1864物理化学性质

[ 分子式 ]:
C₂₅H₂₉Cl₂F₃N₂O₄S

[ 分子量 ]:
581.475

[ 精确质量 ]:
580.117737

[ PSA ]:
90.10000

[ LogP ]:
6.92230

[ 外观性状 ]:
white to beige

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: soluble10mg/mL, clear

EHT 1864MSDS

详细MSDS(安全技术说明书)

EHT 1864安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

EHT 1864文献

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Blood 125(1) , 175-84, (2015)

Akt is an important signaling molecule regulating platelet aggregation. Akt is phosphorylated after translocation to the membrane through Gi signaling pathways by a phosphatidylinositol-3,4,5-trisphos...

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Sci. Signal. 8 , ra114, (2015)

Cytokines dimerize cell surface receptors to activate signaling and regulate many facets of the immune response. Many cytokines have pleiotropic effects, inducing a spectrum of redundant and distinct ...

An integrated imaging approach to the study of oxidative stress generation by mitochondrial dysfunction in living cells.

Environ. Health Perspect. 118 , 902-8, (2010)

The mechanisms of action of many environmental agents commonly involve oxidative stress resulting from mitochondrial dysfunction. Zinc is a common environmental metallic contaminant that has been impl...

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