1. Epigenetics
  2. Epigenetic Reader Domain Histone Acetyltransferase
  3. SGC-CBP30

SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

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

CAS No. : 1613695-14-9

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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

Top Publications Citing Use of Products

    SGC-CBP30 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 28:S2090-1232(24)00624-6.

    SGC-CBP30 (7.5 μg/mL, for 8 days) inhibits adipogenic differentiation in EBF2-overexpressing cells, as assessed by Oil Red O staining.

    SGC-CBP30 purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 28:S2090-1232(24)00624-6.

    SGC-CBP30 (7.5 μg/mL, for 8 days) downregulated the expression of brown fat marker genes (BMP7, CIDEA, and PPARγ) and mitochondrial markers (PGC1α, Cox7a1, and Cox5b) induced in EBF2-overexpressing cells.

    SGC-CBP30 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19.   [Abstract]

    The combination of SGC-CBP30 (0.2 and 0.4 μM, 5 days) and Lenalidomide (10 μM, 5 days) exerted substantial synergy in reducing the viability of myeloma XG1LenRes cells.

    SGC-CBP30 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19.   [Abstract]

    Immunoblotting assays detected the changes in IRF4, MYC, and STAT3 after treatment with Lenalidomide (10 μM) or SGC-CBP30 (0.2 and 0.4 μM) alone or in combination (day 3).

    SGC-CBP30 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19.   [Abstract]

    SGC-CBP30 (0.2 and 0.4 μM, 2 days) treatment also reduced autocrine IL-6 production in XG1LenRes cells, both in the absence and presence of Lenalidomide (10 μM, 2 days).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects[1][2][3].

    IC50 & Target

    CBP/p300

     

    Cellular Effect
    Cell Line Type Value Description References
    CWR22R IC50
    > 10 μM
    Compound: CBP30
    Antiproliferative activity against human 22Rv1 cells incubated for 5 days by CCK-8 method
    Antiproliferative activity against human 22Rv1 cells incubated for 5 days by CCK-8 method
    [PMID: 35569250]
    HEK293 IC50
    2.8 μM
    Compound: 2; SGC-CBP30
    Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incubation by BRET assay
    Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incubation by BRET assay
    [PMID: 27682507]
    MCF7 IC50
    2.39 μM
    Compound: CBP30
    Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 method
    Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 method
    [PMID: 35569250]
    MOLM-13 IC50
    1.53 μM
    Compound: CBP30
    Cytotoxicity against human MOLM-13 cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo luminescence assay
    Cytotoxicity against human MOLM-13 cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo luminescence assay
    [PMID: 33872011]
    OPM-2 IC50
    2.64 μM
    Compound: CBP30
    Antiproliferative activity against human OPM-2 cells incubated for 5 days by CCK-8 method
    Antiproliferative activity against human OPM-2 cells incubated for 5 days by CCK-8 method
    [PMID: 35569250]
    RKO IC50
    1.5 μM
    Compound: 11; SGC-CBP30
    Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin for 16 hrs by luciferase reporter assay
    Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin for 16 hrs by luciferase reporter assay
    [PMID: 26572217]
    SCC-9 IC50
    6.42 μM
    Compound: CBP30
    Antiproliferative activity against human SCC-9 cells incubated for 5 days by CCK-8 method
    Antiproliferative activity against human SCC-9 cells incubated for 5 days by CCK-8 method
    [PMID: 35569250]
    In Vitro

    In ankylosing spondylitis and psoriatic arthritis condition, SGC-CBP30 inhibits IL-17A secretion by Th17 cells. Transcriptional profiling of human T cells after SGC-CBP30 treatment shows a much more restricted effect on gene expression than that observed with the pan-BET (bromo and extraterminal domain protein family) bromodomain inhibitor JQ1[1].

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

    In Vivo

    SGC-CBP30 treatment slightly alleviates alveolar bronchial fibrosis induced by NSC-125066. SGC-CBP30 plus CQ-061 dramatically reduces alveolar bronchial fibrosis. The ELISA of cytokines IL-4 and IFN-γ in BALF demonstrates that combination of SGC-CBP300 and CQ-061 suppresses the activation of IL-4 as well as IFN-γ in NSC-125066 induced IPF murine models to nearly normal levels[2].

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

    Animal Model: Sprague-Dawley (SD) rats (aged 3-4 weeks) injected with NSC-125066[2]
    Dosage: 25 mg/kg
    Administration: Oral administration; daily; for 14 days
    Result: Slightly alleviated alveolar bronchial fibrosis induced by NSC-125066.
    Molecular Weight

    509.04

    Formula

    C28H33ClN4O3

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C42

    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 : 66.67 mg/mL (130.97 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 1.9645 mL 9.8224 mL 19.6448 mL
    5 mM 0.3929 mL 1.9645 mL 3.9290 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)

    Mass
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    Concentration
    ×
    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: ≥ 2.5 mg/mL (4.91 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.83%

    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 1.9645 mL 9.8224 mL 19.6448 mL 49.1121 mL
    5 mM 0.3929 mL 1.9645 mL 3.9290 mL 9.8224 mL
    10 mM 0.1964 mL 0.9822 mL 1.9645 mL 4.9112 mL
    15 mM 0.1310 mL 0.6548 mL 1.3097 mL 3.2741 mL
    20 mM 0.0982 mL 0.4911 mL 0.9822 mL 2.4556 mL
    25 mM 0.0786 mL 0.3929 mL 0.7858 mL 1.9645 mL
    30 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6371 mL
    40 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
    50 mM 0.0393 mL 0.1964 mL 0.3929 mL 0.9822 mL
    60 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
    80 mM 0.0246 mL 0.1228 mL 0.2456 mL 0.6139 mL
    100 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4911 mL
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    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.

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