2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. EHT 1864

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.

For research use only. We do not sell to patients.

CAS No. : 754240-09-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 22 publication(s) in Google Scholar

EHT 1864 Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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.

    EHT 1864 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jun 1:7:364-376.

    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.

    EHT1864 (20 μM) inhibited the increase in YAP nuclear localization induced by PXN overexpression.

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    K-Ras H-Ras N-Ras Ras

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    Description

    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[1][2][3][4].

    In Vivo

    EHT 1864 (oral administration) displays good tolerability, brain penetrance, and no genotoxicity. EHT 1864 (10 and 40 mg/kg/day; daily; 15 days; intraperitoneal injections) lowers brain Aβ 40 by 37% in guinea pigs[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    581.48

    Formula

    C25H29Cl2F3N2O4S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34.[H]Cl.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7197 mL 8.5987 mL 17.1975 mL
    5 mM 0.3439 mL 1.7197 mL 3.4395 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.

    • Protocol 1

      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

    • Protocol 2

      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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.85%

    SDS (393 KB)

    COA (245 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References

    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.

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    EHT 1864 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    EHT 1864754240-09-0EHT1864EHT-1864Rasβ-amyloidamyloidprecursorproteinAlzheimerdiseasetransformationInhibitorinhibitorinhibit

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