Biological Activity
Inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo.
Licensing Information
Sold for research use only under license from ExonHit Therapeutics S.A.
Technical Data
| M. Wt | 581.47 |
| Formula | C25H27F3N2O4S.2HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 754240-09-0 |
| PubChem ID | 9938202 |
| InChI Key | LSECOAJFCKFQJG-UHFFFAOYSA-N |
| Smiles | O=C1C=C(CN4CCOCC4)OC=C1OCCCCCSC3=CC=NC2=CC(C(F)(F)F)=CC=C23.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.61 | 75 | |
| water | 58.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 581.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.72 mL | 8.6 mL | 17.2 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Desire et al (2005) RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo. J.Biol.Chem. 280 37516 PMID: 16150730
Shutes et al (2007) Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases. J.Biol.Chem. 282 35666 PMID: 17932039
Onesto et al (2008) Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 439 111 PMID: 18374160
Keywords: EHT 1864, supplier, Rac-GEF, interaction, antioncogenic, G, Proteins, Small, transformation, Rac1, Rac1b, Rac2, Rac3, Ras, Tiam, inhibits, inhibitors, GTPases, EHT1864, G, Proteins, (Small), GTPase, G, Proteins, (Small), Tocris Bioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。 目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔（Bristol）的高品质试剂提供商，共有2000多种产品，主要集中在神经科学和信号传导领域，产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等，主要产品包括GPCR ligands，神经传递素，离子通道调控剂，信号通路抑制剂等，这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者，其生产的影响神经系统的化学物质被多次引用，这些物质很多都来自Jeff Watkins（Tocris 的创立人）在Bristol大学原创性的研究工作。
Tocris Bioscience has been working with scientists for over 30 years to provide the life science community with the latest and most innovative research tools available. We understand the need for researchers to trust their research reagents, which is why we are committed to supplying our customers with the highest quality product available, so you can publish with confidence. To find out more about Tocris, please click on the tiles below.
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