EHT 1864 2HCl

製品コードS7482 バッチS748201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H29Cl2F3N2O4S
分子量 581.47 CAS No. 754240-09-0
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 100 mg/mL (171.97 mM)
Water 100 mg/mL (171.97 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 EHT 1864 2HClは、Rac1、Rac1b、Rac2、Rac3に対してそれぞれ40 nM、50 nM、60 nM、250 nMのKdを持つ、強力なRacファミリーGTPase阻害剤です。
in vitro EHT 1864 selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1. EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH 3T3 cells stably expressing H-Ras(61L) protein. EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down.
in vivo EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains.

プロトコル(参考用のみ)

キナーゼアッセイ Inhibitor:GTPase binding analyses
For inhibitor:GTPase binding analyses, aliquots of small GTPase solution (containing 1 μM inhibitor) are titrated into a solution of 1 μM inhibitor in the cuvette. Changes in fluorescence anisotropy are monitored at λex = 360 nm, λem = 440 nm, 30 s after each addition. All data analysis and curve fitting were performed using Microsoft Excel and QuantumSoft's ProFit for Mac OS X.
細胞アッセイ 細胞株 NIH 3T3 cells
濃度 ~5 μM
反応時間 4 days
実験の流れ NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.
動物実験 動物モデル Male Hartley albino guinea pigs
投薬量 40 mg/kg daily
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17932039/
  • https://pubmed.ncbi.nlm.nih.gov/16150730/
  • https://pubmed.ncbi.nlm.nih.gov/24352656/

カスタマーフィードバック

Data from [Data independently produced by , , FASEB J, 2018, 32(4):2197-2211]

Data from [Data independently produced by , , Am J Cancer Res, 2018, 8(1):70-80]

Data from [Data independently produced by , , Mol Biol Cell, 2017, 28(13):1745-1753]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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