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

A-485 

Cat. No.: HY-107455 Purity: 99.08%
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
10 mM * 1  mL in DMSO USD 266 In-stock
Estimated Time of Arrival: December 31
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  

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Customer Review

Based on 2 publication(s) in Google Scholar

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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].

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].

Molecular Weight

536.48

Formula

C₂₅H₂₄F₄N₄O₅

CAS No.

1889279-16-6

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 : 100 mg/mL (186.40 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:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.5 mg/mL (6.52 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3.5 mg/mL (6.52 mM); Clear solution

  • 3.

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

    Solubility: ≥ 3.5 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 99.08%

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Keywords:

A-485A485A 485Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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Product Name:
A-485
Cat. No.:
HY-107455
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