1. Epigenetics
  2. Epigenetic Reader Domain Histone Acetyltransferase
  3. A-485

A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.

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

A-485 Chemical Structure

A-485 Chemical Structure

CAS No. : 1889279-16-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 266 In-stock
Solution
10 mM * 1 mL in DMSO USD 266 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 225 In-stock
10 mg USD 390 In-stock
50 mg USD 545 In-stock
100 mg USD 940 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 42 publication(s) in Google Scholar

Top Publications Citing Use of Products

40 Publications Citing Use of MCE A-485

WB

    A-485 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Jan;24(1):162-173.  [Abstract]

    A485 (10 μM; 24 h) leads to the downregulation of H3K9bhb and CPS1 in BHB-treated CD8+ TM cells; however, the use of 3-TYP (10 μM; 24 h) or Trichostatin A (TSA; 5 nM; 24 h) result in the increase of H3K9bhb and CPS1.

    A-485 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Feb 13;160:114402.  [Abstract]

    A485 (1, 3 µM; 4 h) reduces endogenous acetylation of NPM1 in HA-NPM1-transfected Huh7/SR NPM1 KD cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively[1].

    IC50 & Target

    IC50: 9.8 nM (p300), 2.6 nM (CBP)[1]

    In Vitro

    A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC50) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.
    The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines[1].

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

    In Vivo

    After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen[1].

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

    Molecular Weight

    536.48

    Formula

    C25H24F4N4O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1CC(N([C@@H](C)C(F)(F)F)CC2=CC=C(F)C=C2)=O)[C@]3(OC1=O)C4=CC=C(NC(NC)=O)C=C4CC3

    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 : 125 mg/mL (233.00 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 1.8640 mL 9.3200 mL 18.6400 mL
    5 mM 0.3728 mL 1.8640 mL 3.7280 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
    =
    Concentration
    ×
    Volume
    ×
    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 11 mg/mL (20.50 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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
    Cell Assay
    [1]

    Cell lines are plated in 96 well or 384 well plates and allowed to adhere for 24 h. The cells are then treated with A-485 for 3, 4, or 5 days. Experiments are run in triplicate and the fraction of viable cells is determined using the Cell Viability Assay according to the manufacturer’s recommendations. For Thymidine incorporation assays, cells are treated with A-485 for 1, 2, 3, or 4 days. Twenty four hours prior to the time point, tritiated thymidine is added and cells are incubated for an additional 24 h. Genomic DNA is then isolated on filter plates[1].

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

    Animal Administration
    [1]

    The LuCap-77 CR prostate PDX model is used in this study. Donor tumors are dissociated and injected as a brie (1:2) into the right flank of 16 week old male C.B.-17 SCID mice on day 0 in a volume of 0.2 mL. Tumors are size matched on day 26 post-inoculation with a mean tumor volume of 211±3 (SEM) mm3 with dosing beginning on day 28. Mice are randomized into treatment groups using Studylog software based on tumor volume. LuCap-77 CR xenograft tumors are established in SCID mice and animals are dosed with A-485 as for 7 days. Three hours post the final dose, tumors are harvested and snap frozen on dry ice[1].

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

    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 1.8640 mL 9.3200 mL 18.6400 mL 46.6001 mL
    5 mM 0.3728 mL 1.8640 mL 3.7280 mL 9.3200 mL
    10 mM 0.1864 mL 0.9320 mL 1.8640 mL 4.6600 mL
    15 mM 0.1243 mL 0.6213 mL 1.2427 mL 3.1067 mL
    20 mM 0.0932 mL 0.4660 mL 0.9320 mL 2.3300 mL
    25 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8640 mL
    30 mM 0.0621 mL 0.3107 mL 0.6213 mL 1.5533 mL
    40 mM 0.0466 mL 0.2330 mL 0.4660 mL 1.1650 mL
    50 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9320 mL
    60 mM 0.0311 mL 0.1553 mL 0.3107 mL 0.7767 mL
    80 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5825 mL
    100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4660 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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    Product Name:
    A-485
    Cat. No.:
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