EHT 1864
Based on 23 publication(s) in Google Scholar
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.85%
- CAS 番号: 754240-09-0
- 分子式: C25H29Cl2F3N2O4S
- 分子量:581.48
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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MedChemExpress（MCE）の使用を引用している文献 EHT 1864
More- Bioact Mater. 2021 Jun 1:7:364-376. [Abstract]
- Adv Sci (Weinh). 2025 Jun 23:e03322. [Abstract]
- Sci Adv. 2023 May 24;9(21):eadg1778. [Abstract]
- Cell Rep. 2025 Dec 6;44(12):116649. [Abstract]
- Cell Rep. 2025 Mar 5;44(3):115397. [Abstract]
- Front Immunol. 2018 Aug 31:9:1987. [Abstract]
- Eur J Pharmacol. 2024 Jul 5:974:176608. [Abstract]
- J Pathol. 2017 Oct;243(2):208-219. [Abstract]
- J Mol Med (Berl). 2023 Dec;101(12):1567-1585. [Abstract]
- PLoS Pathog. 2024 Nov 21;20(11):e1012681. [Abstract]
- Cell Signal. 2022 Aug:96:110358. [Abstract]
- J Virol. 2025 Jun 25:e0063825. [Abstract]
- J Med Virol. 2024 Dec;96(12):e70138. [Abstract]
- J Leukoc Biol. 2025 Jan 30:qiaf012. [Abstract]
- PLoS One. 2022 Jun 24;17(6):e0270197. [Abstract]
- Cancer Genomics Proteomics. 2026 May-Jun;23(3):407-429. [Abstract]
- bioRxiv. 2026 Jan 2.
- University of California. 2025.
- bioRxiv. 2025 Jul 18:2025.07.14.664742. [Abstract]
- Free University of Berlin. 2024.
- bioRxiv. 2023 Oct 16.
- bioRxiv. January 12, 2022.
- Evid Based Complement Alternat Med. 2020 Apr 29;2020:2760979. [Abstract]
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生物活性
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 754240-09-0
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性状 Solid
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分子量 581.48
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分子式 C25H29Cl2F3N2O4S
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Color White to off-white
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SMILES
O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34.[H]Cl.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (23)
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Journal Impact Factor
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Most Recent
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Bioact Mater
2021 Jun 1:7:364-376. PMID: 34466738
EHT 1864 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jun 1:7:364-376. [Abstract]
EHT1864 (20 μM) treatment inhibited PXN overexpression-induced cell stiffness.
EHT 1864 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jun 1:7:364-376. [Abstract]
EHT1864 (20 μM) inhibited the increase in YAP nuclear localization induced by PXN overexpression.
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Adv Sci (Weinh)
Splicing Shift of RAC1 Accelerates Tumorigenesis and Defines a Potent Therapeutic Target in Lung Cancer. [Abstract]2025 Jun 23:e03322. PMID: 40548642 -
Sci Adv
Neuropilin 1 is an entry receptor for KSHV infection of mesenchymal stem cell through TGFBR1/2-mediated macropinocytosis. [Abstract]2023 May 24;9(21):eadg1778. PMID: 37224259
EHT 1864 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 May 24;9(21):eadg1778. [Abstract]
Cdc42 or Rac1 inhibitors can inhibit KSHV endocytosis. PDLSCs pretreated with MLS-573151 or EHT1864 for 15 minutes were infected with KSHV at 37°C for 4 hours, followed by relative quantitative real-time PCR analysis to detect KSHV copy number.
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Cell Rep
Context-dependent inhibitory roles of RhoA in 3D invasive cell migration within the extracellular matrix. [Abstract]2025 Dec 6;44(12):116649. PMID: 41359424
EHT 1864 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Dec 6;44(12):116649. [Abstract]
Single wild-type (WT) and RHOA knockout (RHOA-KO) HEK293 cells were seeded in Geltrex medium and cultured for 4 days in the presence of 10 μM EHT1864.
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Cell Rep
ENKD1 modulates innate immune responses through enhanced geranylgeranyl pyrophosphate synthase activity. [Abstract]2025 Mar 5;44(3):115397. PMID: 40048432
EHT 1864 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Mar 5;44(3):115397. [Abstract]
IL-6 and TNF-α protein levels in Enkd1fl/fl and Enkd1Δmye BMDMs pretreated with EHT 1864, followed by stimulation with or without LPS.
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Front Immunol
Cytotoxic Necrotizing Factor 1 Downregulates CD36 Transcription in Macrophages to Induce Inflammation During Acute Urinary Tract Infections. [Abstract]2018 Aug 31:9:1987. PMID: 30233583 -
Eur J Pharmacol
Cycloheptylprodigiosin from marine bacterium Spartinivicinus ruber MCCC 1K03745T induces a novel form of cell death characterized by Golgi disruption and enhanced secretion of cathepsin D in non-small cell lung cancer cell lines. [Abstract]2024 Jul 5:974:176608. PMID: 38663542 -
J Pathol
Cytotoxic necrotizing factor 1 promotes prostate cancer progression through activating the Cdc42-PAK1 axis. [Abstract]2017 Oct;243(2):208-219. PMID: 28707808 -
J Mol Med (Berl)
Vav2 promotes ductus arteriosus anatomic closure via the remodeling of smooth muscle cells by Rac1 activation. [Abstract]2023 Dec;101(12):1567-1585. PMID: 37804474 -
PLoS Pathog
Massive entry of BK Polyomavirus induces transient cytoplasmic vacuolization of human renal proximal tubule epithelial cells. [Abstract]2024 Nov 21;20(11):e1012681. PMID: 39570904 -
Cell Signal
BTK-independent regulation of calcium signalling downstream of the B-cell receptor in malignant B-cells. [Abstract]2022 Aug:96:110358. PMID: 35597428 -
J Virol
Rabies virus utilizes neuropilin 2 as an endocytic receptor to trigger TGFBR1-mediated actin polymerization. [Abstract]2025 Jun 25:e0063825. PMID: 40558096 -
J Med Virol
2024 Dec;96(12):e70138. PMID: 39717911 -
J Leukoc Biol
Nexinhib20 inhibits JFC1-mediated mobilization of a subset of CD11b/CD18+ vesicles decreasing integrin avidity, but does not inhibit Rac1. [Abstract]2025 Jan 30:qiaf012. PMID: 39883854 -
PLoS One
Human endothelial cells display a rapid tensional stress increase in response to tumor necrosis factor-α. [Abstract]2022 Jun 24;17(6):e0270197. PMID: 35749538 -
Cancer Genomics Proteomics
Integrated Proteomics Reveal ALDH1A1 as an Oncogenic Driver and Regulatory Hub in Hepatocellular Carcinoma. [Abstract]2026 May-Jun;23(3):407-429. PMID: 42055623 -
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bioRxiv
PP2A activation drives aberrant macropinocytosis and cell death in pancreatic ductal adenocarcinoma. [Abstract]2025 Jul 18:2025.07.14.664742. PMID: 40791444 -
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Evid Based Complement Alternat Med
Ethanol Extract of the Infructescence of Platycarya strobilacea Sieb. et Zucc. Induces Methuosis of Human Nasopharyngeal Carcinoma Cells. [Abstract]2020 Apr 29;2020:2760979. PMID: 32419796
溶剤 & 溶解度
H2O : ≥ 100 mg/mL (171.97 mM)
DMSO : ≥ 32 mg/mL (55.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (42.99 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Add each solvent one by one: Saline
Solubility: 25 mg/mL (42.99 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Ying Liu , et al. Podocyte-Released Migrasomes in Urine Serve as an Indicator for Early Podocyte Injury. Kidney Dis (Basel). 2020 Nov;6(6):422-433. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.7197 mL | 8.5987 mL | 17.1975 mL | 42.9937 mL |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4395 mL | 8.5987 mL | |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7197 mL | 4.2994 mL | |
| 15 mM | 0.1146 mL | 0.5732 mL | 1.1465 mL | 2.8662 mL | |
| 20 mM | 0.0860 mL | 0.4299 mL | 0.8599 mL | 2.1497 mL | |
| 25 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL | |
| 30 mM | 0.0573 mL | 0.2866 mL | 0.5732 mL | 1.4331 mL | |
| 40 mM | 0.0430 mL | 0.2150 mL | 0.4299 mL | 1.0748 mL | |
| 50 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8599 mL | |
| H2O | 60 mM | 0.0287 mL | 0.1433 mL | 0.2866 mL | 0.7166 mL |
| 80 mM | 0.0215 mL | 0.1075 mL | 0.2150 mL | 0.5374 mL | |
| 100 mM | 0.0172 mL | 0.0860 mL | 0.1720 mL | 0.4299 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
EHT 1864 関連分類
HY-16659 関連分類
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