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

A-485 

Cat. No.: HY-107455 Purity: 99.90%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 266 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 266 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 225 In-stock
Estimated Time of Arrival: December 31
10 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 545 In-stock
Estimated Time of Arrival: December 31
100 mg USD 940 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 24 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A-485 purchased from MCE. 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 MCE. 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].

    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].

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

    536.48

    Appearance

    Solid

    Formula

    C25H24F4N4O5
    CAS No.
    SMILES

    O=C(N1CC(N([[email protected]@H](C)C(F)(F)F)CC2=CC=C(F)C=C2)=O)[[email protected]]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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (233.00 mM; Need ultrasonic)

    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
    10 mM 0.1864 mL 0.9320 mL 1.8640 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.90%

    COA (250 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    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
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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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    Keywords:

    A-4851889279-16-6A485A 485Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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