2. Metabolic Enzyme/Protease
  3. Glutamate Dehydrogenase (GLDH)
  4. R162

R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.

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

CAS No. : 64302-87-0

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of R162:

R162 Related Antibodies

Top Publications Citing Use of Products

    R162 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Feb;12(2):759-773.

    R162 (20 μM, 48 h) inhibited GDH1 and resulted in greatly increased cell apoptosis.

    R162 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Feb;12(2):759-773.

    CAI, CB-839, or R162 (20 μM, 48 h) alone slightly increased the generation of intracellular ROS, whereas ROS generation was significantly increased in the combination group.

    R162 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Feb;12(2):759-773.

    Western blots showing the expressions of caspase 3, cleaved caspase 3, caspase 6, cleaved caspase 6, caspase 7 and cleaved caspase 7 after 48 h of CAI (10 μmol/L), CB-839 (100 nmol/L), CAI + CB-839, R162 (20 μmol/L) or CAI + R162.

    R162 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Feb;12(2):759-773.

    The ratio of GSH to GSSG in HCT116 cells and C26 cells with CAI (10 μmol/L), CB-839 (100 nmol/L), CAI + CB-839, R162 (20 μmol/L) or CAI + R162 for 48 h.

    R162 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Feb;12(2):759-773.

    Nude mice bearing 5 mm × 5 mm C26 cell tumors were treated with PBS, CAI (20 mg/kg), CB-839 (200 mg/kg), or CAI/CB-839 or PBS, CAI, R162 (20 mg/kg), or CAI/R162 for 21 days. The tumor growth curves of tumor-bearing mice receiving various treatments.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.

    In Vitro

    Inhibition of GDH1 activity by R162 treatment results in decreased intracellular fumarate levels, attenuated GPx activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells, which can be significantly rescued by methyl-α-KG treatment as well as by antioxidant NAC. R162 inhibits cell proliferation and tumor growth potential of human cancer cells[1].

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

    R162 Related Antibodies
    In Vivo

    R162 (30 mg/kg/day, i.p.) does not result in a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties in xenograft tumor mouse models. R162 (20 mg/kg/day) results in significantly decreased tumor growth and masses in mice compared with control mice and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice[1].

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

    264.28

    Formula

    C17H12O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C2=C(C=CC=C2)C(C3=CC=C(CC=C)C(O)=C13)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (37.84 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)

    Ethanol : 1 mg/mL (3.78 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7839 mL 18.9193 mL 37.8387 mL
    5 mM 0.7568 mL 3.7839 mL 7.5677 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

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

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.98%

    SDS (393 KB)

    COA (248 KB) HNMR (431 KB) LCMS (95 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 3.7839 mL 18.9193 mL 37.8387 mL 94.5966 mL
    DMSO 5 mM 0.7568 mL 3.7839 mL 7.5677 mL 18.9193 mL
    10 mM 0.3784 mL 1.8919 mL 3.7839 mL 9.4597 mL
    15 mM 0.2523 mL 1.2613 mL 2.5226 mL 6.3064 mL
    20 mM 0.1892 mL 0.9460 mL 1.8919 mL 4.7298 mL
    25 mM 0.1514 mL 0.7568 mL 1.5135 mL 3.7839 mL
    30 mM 0.1261 mL 0.6306 mL 1.2613 mL 3.1532 mL
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    R162 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:

    R16264302-87-0R 162R-162Glutamate Dehydrogenase (GLDH)Glutamate DehydrogenaseInhibitorinhibitorinhibit

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