2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Dehydrogenase (PHGDH)
  4. CBR-5884

CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.

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

CAS No. : 681159-27-3

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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 20 publication(s) in Google Scholar

CBR-5884 Related Antibodies

Top Publications Citing Use of Products

    CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Mar 16;44(3):115426.  [Abstract]

    CBR-5884 (15 μM; 6 h) increases PA-induced TAK1 activation and proinflammatory cytokine expression.

    CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Nov;19(11):1263-1278.  [Abstract]

    PHGDH inhibits M(IFN-γ) but promotes M(IL-4) polarization through its enzymatic activity. Wild-type bone marrow-derived macrophages (BMDMs) were pretreated with the PHGDH inhibitor CBR-5884 (15 μM) for 12 h and were then stimulated with IFN-γ (100 ng/ml) for 12 h followed by qRT-PCR analysis of M1.

    CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Nov;19(11):1263-1278.  [Abstract]

    PHGDH inhibits M(IFN-γ) but promotes M(IL-4) polarization through its enzymatic activity. Wild-type bone marrow-derived macrophages (BMDMs) were pretreated with the PHGDH inhibitor CBR-5884 (15 μM) for 12 h and were then stimulated with IFN-γ (100 ng/ml) for 12 h followed by western blot analysis of M1.

    CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 May 4;33(5):971-987.e6.  [Abstract]

    WT PMs were pretreated with the PHGDH inhibitor CBR-5884 (15 μM or 30 μM) for 12 h and then infected with VSV for western blot detection of p-IRF3(S396), IRF3, p-TBK1(S172), and TBK1.

    CBR-5884 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jun 20;10(1):2701.  [Abstract]

    Sensitivity to PHGDH inhibition. Cell viability was measured using CCK-8 assay after treatment with CBR5884 (20 µM) for 72 h. Data were means of triplicates; error bars represented SD.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis[1].

    IC50 & Target

    PHGDH, serine synthesis[1]
    Cellular Effect
    Cell Line Type Value Description References
    MCF-10A IC50
    57.2 μM
    Compound: 6; CBR-5884
    Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay
    		[PMID: 36594670]
    MDA-MB-468 IC50
    20.9 μM
    Compound: 6; CBR-5884
    Antiproliferative activity against human MDA-MB-468 cells expressing PHGDH assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MDA-MB-468 cells expressing PHGDH assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay
    		[PMID: 36594670]
    In Vitro

    CBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.

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

    CBR-5884 Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: Breast and melanoma cell lines
    Concentration: 15 or 30 μM
    Incubation Time: 3-5 days
    Result: Inhibited the proliferation of melanoma and breast cancer lines.
    Molecular Weight

    336.39

    Formula

    C14H12N2O4S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=C(C)C(SC#N)=C(NC(C2=CC=CO2)=O)S1)OCC
    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 : 50 mg/mL (148.64 mM; Need ultrasonic; 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 2.9727 mL 14.8637 mL 29.7274 mL
    5 mM 0.5945 mL 2.9727 mL 5.9455 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

    • 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    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (6.18 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  15% Cremophor EL    85% Saline

      Solubility: 7 mg/mL (20.81 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.02%

    SDS (393 KB)

    COA (252 KB) HNMR (237 KB) LCMS (123 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
    DMSO 1 mM 2.9727 mL 14.8637 mL 29.7274 mL 74.3185 mL
    5 mM 0.5945 mL 2.9727 mL 5.9455 mL 14.8637 mL
    10 mM 0.2973 mL 1.4864 mL 2.9727 mL 7.4318 mL
    15 mM 0.1982 mL 0.9909 mL 1.9818 mL 4.9546 mL
    20 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7159 mL
    25 mM 0.1189 mL 0.5945 mL 1.1891 mL 2.9727 mL
    30 mM 0.0991 mL 0.4955 mL 0.9909 mL 2.4773 mL
    40 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
    50 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4864 mL
    60 mM 0.0495 mL 0.2477 mL 0.4955 mL 1.2386 mL
    80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
    100 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
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    CBR-5884 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:

    CBR-5884681159-27-3CBR5884CBR 5884Phosphoglycerate Dehydrogenase (PHGDH)Inhibitorinhibitorinhibit

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