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  3. Inobrodib

Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.

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

CAS No. : 2222941-37-7

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Inobrodib:

Top Publications Citing Use of Products

    Inobrodib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jun 3;16(1):432.  [Abstract]

    Western blot and qRT-PCR analyses were performed to evaluate the PD-L1 levels in RCC10 and RCC4 cells treated with DMF/FHIN1, both in the absence and presence of 20 μM A485 or 100 nM CCS1477, an inhibitor of p300.

    Inobrodib purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2025 Oct;26(19):4766-4793.  [Abstract]

    RT-qPCR for eRNA of NKX2-2, CCND1 and PPP1R1A enhancers following 6 h treatment of A-485, CCS1477 (1 μM), and dCBP-1 treatment in SKNMC cells.

    Inobrodib purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2025 Oct;26(19):4766-4793.  [Abstract]

    Cell viability of SKNMC and A673 cells treated with A-485, CCS1477 (1 μM) and Dual combination for 6 days measured by CellTiter-Glo.

    Inobrodib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 5;15(1):4770.  [Abstract]

    IC50 values of the CBP/p300 inhibitors CP-C27, A-485, and Inobrodib (6 days), the EZH2 inhibitor tazemetostat, and the EZH1/EZH2 inhibitor valemetostat in HEK293T, JMU-RTK-2 +SMARCB1, and JMU-RTK-2 -SMARCB1 cells.

    Inobrodib purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 Jan 25;52(2):625-642.  [Abstract]

    Bar graphs depict KLK3 gene expression analysis in VCaP ENZ 0, VCaP ENZ 3w, 22Rv1 ENZ 0, and 22Rv1 ENZ 3w cells treated with or without Dex in the presence or absence of 0.1 or 1 μM of indicated inhibitor (A-485, CCS1477, I-BET762, BRM014).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression[1].

    IC50 & Target

    p300/CBP[1]

    Cellular Effect
    Cell Line Type Value Description References
    CWR22R IC50
    0.42 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay
    Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay
    [PMID: 34962793]
    CWR22R IC50
    184 nM
    Compound: 3; CCS1477
    Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    [PMID: 38530938]
    CWR22R IC50
    184 nM
    Compound: 5; CCS1477
    Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    [PMID: 38477974]
    EOL1 IC50
    < 3 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human EOL1 cells
    Antiproliferative activity against human EOL1 cells
    [PMID: 38649304]
    Hep 3B2 IC50
    1.928 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    Antiproliferative activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    [PMID: 39356741]
    HepG2 IC50
    0.869 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    [PMID: 39356741]
    KG-1 IC50
    17.04 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    [PMID: 38829718]
    KG-1 IC50
    < 3 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human KG-1 cells
    Antiproliferative activity against human KG-1 cells
    [PMID: 38649304]
    L02 IC50
    20 μM
    Compound: 4; CCS1477
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    [PMID: 38829718]
    LNCaP IC50
    0.06 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay
    Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay
    [PMID: 34962793]
    LNCaP IC50
    412 nM
    Compound: 3; CCS1477
    Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    [PMID: 38530938]
    LNCaP IC50
    412 nM
    Compound: 5; CCS1477
    Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    [PMID: 38477974]
    LNCaP C4-2B IC50
    1.65 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay
    Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay
    [PMID: 34962793]
    MOLM-13 IC50
    102.5 nM
    Compound: 4; CCS1477
    Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay
    [PMID: 38649304]
    MOLM-16 IC50
    0.37 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo luminescence analysis
    [PMID: 38829718]
    MOLM-16 IC50
    12.9 nM
    Compound: 4; CCS1477
    Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay
    [PMID: 38649304]
    MOLT-4 IC50
    0.247 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    [PMID: 39356741]
    MV4-11 IC50
    0.014 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 120 hrs by celltiter glo luminescence analysis
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 120 hrs by celltiter glo luminescence analysis
    [PMID: 38829718]
    MV4-11 IC50
    20.4 nM
    Compound: 4; CCS1477
    Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay
    [PMID: 38649304]
    OPM-2 IC50
    30 nM
    Compound: 4; CCS1477
    Antiproliferative activity against human OPM-2 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
    Antiproliferative activity against human OPM-2 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
    [PMID: 39356741]
    RPMI-8226 IC50
    0.082 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
    [PMID: 39356741]
    SK-HEP1 IC50
    4.679 μM
    Compound: 1; CCS1477
    Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
    Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
    [PMID: 38316017]
    THP-1 IC50
    < 3 μM
    Compound: 4; CCS1477
    Antiproliferative activity against human THP-1 cells
    Antiproliferative activity against human THP-1 cells
    [PMID: 38649304]
    VCaP IC50
    195 nM
    Compound: 5; CCS1477
    Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay
    [PMID: 38477974]
    VCaP IC50
    53.6 nM
    Compound: 3; CCS1477
    Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
    [PMID: 38530938]
    In Vitro

    Inobrodib binding to cellular histones in an in-cell BRET assay gives an IC50 of 19 nM for p300 and 1060 nM for BRD4. Inobrodib shows potent growth-inhibitory activity in VCaP, 22Rv1, and LNCaP95 (all IC50 < 100 nM) that express both AR-FL and AR-V7[1].
    ? Inobrodib (0-3000 nM; 48 hours) reduces expression of AR-regulated genes (KLK2, KLK3, and TMPRSS2) in both 22Rv1 and LNCaP95 cells. Inobrodib also reduces C-MYC protein expression in both 22Rv1 and LNCaP95 cells and AR-V7 protein expression in 22Rv1 cells, without clear impact on AR-FL protein expression in 22Rv1 and LNCaP95 cells. Inobrodib reduces C-MYC mRNA and downstream AR and C-MYC signaling in 22Rv1 and C4-2 cells at 16 hours. Inobrodib regulates AR signaling by affecting the recruitment of CBP, p300, and AR-FL to known AR binding sites, and has the potential to abrogate persistent AR signaling in CRPC[1].

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

    In Vivo

    Inobrodib (10-30 mg/kg; oral gavage; 10 or 20 mg/kg daily (QD) or 30 mg/kg every other day (QOD) for 28 days) suppresses growth of a 22Rv1 mouse xenograft model with associated reduction in AR signaling[1].
    ? Inobrodib (20 mg/kg; oral gavage; daily for 8 days) decreases AR and AR-V7 signaling and inhibits growth in a patient- derived model of lethal prostate cancer (NOD/SCID gamma (NSG) male castrated mice)[1].

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

    Animal Model: Noncastrated male athymic nude mice[1]
    Dosage: 10-30 mg/kg
    Administration: Oral gavage; at 10 or 20 mg/kg daily (QD) or at 30 mg/kg every other day (QOD) for 28 days
    Result: Affected tumor growth at 10 mg/kg daily, 20 mg/kg daily, and 30 mg/kg every other day.
    Clinical Trial
    Molecular Weight

    534.60

    Formula

    C30H32F2N4O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1N(C2=CC=C(F)C(F)=C2)[C@H](C3=NC4=CC(C5=C(C)ON=C5C)=CC=C4N3[C@H]6CC[C@H](OC)CC6)CCC1

    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 : 100 mg/mL (187.06 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 1.8706 mL 9.3528 mL 18.7056 mL
    5 mM 0.3741 mL 1.8706 mL 3.7411 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)

    C1

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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 (4.68 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 (4.68 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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

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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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    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: 99.95%

    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 1.8706 mL 9.3528 mL 18.7056 mL 46.7639 mL
    5 mM 0.3741 mL 1.8706 mL 3.7411 mL 9.3528 mL
    10 mM 0.1871 mL 0.9353 mL 1.8706 mL 4.6764 mL
    15 mM 0.1247 mL 0.6235 mL 1.2470 mL 3.1176 mL
    20 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3382 mL
    25 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8706 mL
    30 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
    40 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
    50 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
    60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
    80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5845 mL
    100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4676 mL
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      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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    Product Name:
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    Cat. No.:
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