2. Metabolic Enzyme/Protease
  3. Aminotransferases (Transaminases)
  4. ERG240

ERG240 is an oral active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. ERG240 can be used for the research of cancer, rheumatoid arthritis, and bone disease.

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

CAS No. : 1415683-79-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 5 publication(s) in Google Scholar

ERG240 Related Antibodies

Top Publications Citing Use of Products

    ERG240 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Mar 17:S2090-1232(25)00186-9.  [Abstract]

    OVCAR8-Persister (left) and A2780-Persister (right) cells were pretreated with vehicle, ST1326 (20 μM), ERG240 (60 μM) or IACS-010759 (2 nM) for 24 h and subsequently treated with paclitaxel for 48 h, and cell viability was assessed using a CCK-8 assay or CellTiter-Glo® assay.

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    Description

    ERG240 is an oral active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. ERG240 can be used for the research of cancer, rheumatoid arthritis, and bone disease[1].

    In Vitro

    ERG240 (20 µM, 3 hours) significantly reduces Irg1 mRNA and protein levels, along with itaconate production, in human monocyte-derived macrophages[2].
    ERG240 (5 µM and 10 µM, 24 hours) significantly inhibits migration in bone marrow-derived macrophages (BMDMs)[2].

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

    ERG240 Related Antibodies

    Western Blot Analysis[2]

    Cell Line: Human monocyte-derived macrophages (hMDMs)
    Concentration: 20 µM
    Incubation Time: 3 hours
    Result: Resulted in a significant reduction in IRG1 and IL-1β protein levels, with no significant change in HIF1A and ACTB expression.

    Cell Migration Assay [2]

    Cell Line: Bone Marrow-Derived Macrophages (BMDMs)
    Concentration: 5 µM and 10 µM
    Incubation Time: 24 hours
    Result: Inhibited BMDM migration in a dose-dependent manner without affecting cell viability.

    Real Time qPCR[2]

    Cell Line: Human monocyte-derived macrophages (hMDMs)
    Concentration: 20 µM
    Incubation Time: 3 hours
    Result: Significantly reduced Irg1 mRNA levels, along with itaconate production, without affecting HIF1A and IL1B mRNA levels.
    In Vivo

    ERG240 (500 mg/kg, i.p., administered 30 min before and 8 h after LPS injection) significantly decreases pro-inflammatory response and increases anti-inflammatory transcriptomic features in LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2].
    ERG240 (720 mg/kg and 1000 mg/kg, p.o., once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg)) significantly alleviates inflammation and joint destruction in the collagen-induced arthritis DBA/1 mouse model[2].
    ERG240 (500 mg/kg, p.o., once daily for 10 days) significantly reduces the severity of inflammation and interstitial fibrosis in the NTN WKY rat model induced by nephrotoxic serum[2].

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

    Animal Model: LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2]
    Dosage: 500 mg/kg
    Administration: Intraperitoneal injection (i.p.), administered 30 min before and 8 h after LPS injection
    Result: Reduced Irg1 mRNA and protein levels along with itaconate production.
    Animal Model: Collagen (HY-NP102)-induced arthritis (CIA) DBA/1 mouse model[2]
    Dosage: 720 and 1000 mg/kg
    Administration: Oral gavage (p.o.), once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg)
    Result: Significantly reduced inflammation, cartilage damage, pannus formation, and bone resorption in CIA model; decreased serum levels of pro-inflammatory markers TNF and RANKL.
    Animal Model: Nephrotoxic nephritis (NTN) WKY rat model induced by nephrotoxic serum (NTS) injection[2]
    Dosage: 500 mg/kg
    Administration: Oral gavage (p.o.), once daily for 10 days
    Result: Reduced glomerular crescent formation, proteinuria, serum creatinine, and collagen type I levels.
    Molecular Weight

    166.15

    Formula

    C7H11NaO3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(CCC(C)C(C)=O)O[Na]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

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

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (601.87 mM; Need ultrasonic)

    DMSO : 25 mg/mL (150.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 6.0187 mL 30.0933 mL 60.1866 mL
    5 mM 1.2037 mL 6.0187 mL 12.0373 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.5 mg/mL (15.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (15.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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: 98.0%

    SDS (252 KB)

    COA (244 KB) HNMR (238 KB) MS (71 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 6.0187 mL 30.0933 mL 60.1866 mL 150.4665 mL
    5 mM 1.2037 mL 6.0187 mL 12.0373 mL 30.0933 mL
    10 mM 0.6019 mL 3.0093 mL 6.0187 mL 15.0466 mL
    15 mM 0.4012 mL 2.0062 mL 4.0124 mL 10.0311 mL
    20 mM 0.3009 mL 1.5047 mL 3.0093 mL 7.5233 mL
    25 mM 0.2407 mL 1.2037 mL 2.4075 mL 6.0187 mL
    30 mM 0.2006 mL 1.0031 mL 2.0062 mL 5.0155 mL
    40 mM 0.1505 mL 0.7523 mL 1.5047 mL 3.7617 mL
    50 mM 0.1204 mL 0.6019 mL 1.2037 mL 3.0093 mL
    60 mM 0.1003 mL 0.5016 mL 1.0031 mL 2.5078 mL
    80 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8808 mL
    100 mM 0.0602 mL 0.3009 mL 0.6019 mL 1.5047 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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    ERG240 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:

    ERG2401415683-79-2ERG 240ERG-240Aminotransferases (Transaminases)branched-chain amino acid aminotransferase 1 (BCAT1)cancerrheumatoid arthritisbone diseaseInhibitorinhibitorinhibit

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