A-485

Name: A-485
Brand: MedChemExpress
SKU: HY-107455
Rating: 5.0 (55 reviews)

Cat. No.: HY-107455 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1889279-16-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 266	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	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

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Customer Review

Based on 55 publication(s) in Google Scholar

53 Publications Citing Use of MCE A-485

: 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⁺ T_M 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.

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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

CBP/p300

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	490 nM Compound: A-485	Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
K562	IC₅₀	457 nM Compound: A-485	Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
Kasumi 1	EC₅₀	0.33 μM Compound: A-485	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability incubated for 5 days by XTT assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability incubated for 5 days by XTT assay	[PMID: 32314924]
Kasumi 1	IC₅₀	607.9 nM Compound: A-485	Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
LNCaP	EC₅₀	0.26 μM Compound: A-485	Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
LNCaP-Clone-FGC	EC₅₀	0.35 μM Compound: 1; A-485	Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method	[PMID: 34055218]
LNCaP-Clone-FGC	IC₅₀	215 nM Compound: A-485	Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay	[PMID: 31910017]
Maver1	IC₅₀	226.1 nM Compound: A-485	Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
MCF7	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis	[PMID: 32314924]
MCF7	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human tamoxifen-resistant MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis Antiproliferative activity against human tamoxifen-resistant MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis	[PMID: 32314924]
MDA-MB-231	EC₅₀	> 10 μM Compound: A-485	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
MM1.S	EC₅₀	139 nM Compound: A-485	Antiproliferative activity against human MM1.S cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay Antiproliferative activity against human MM1.S cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay	[PMID: 35814928]
MOLM-13	EC₅₀	0.35 μM Compound: A-485	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
MV4-11	IC₅₀	255.2 nM Compound: A-485	Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
OVCAR-3	EC₅₀	5.44 μM Compound: A-485	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 120 hrs by Cell-titre glo assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 120 hrs by Cell-titre glo assay	[PMID: 34801827]
PANC-1	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 32314924]
PC-3	EC₅₀	2.1 μM Compound: A-485	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
RPMI-8226	EC₅₀	0.16 μM Compound: A-485	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
Sf9	IC₅₀	0.06 μM Compound: A-485	Inhibition of recombinant human N-terminal 6His-FLAG-tagged p300 BHC domain (1036 to 1822 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H4 peptide as substrate preincubated for 30 mins followed by substrate additi Inhibition of recombinant human N-terminal 6His-FLAG-tagged p300 BHC domain (1036 to 1822 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H4 peptide as substrate preincubated for 30 mins followed by substrate additi	[PMID: 31910017]

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.

1889279-16-6

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
10 mM	0.1864 mL	0.9320 mL	1.8640 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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 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

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 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

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: 99.87%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132. [Content Brief]

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	[1]. Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132. [Content Brief]

Complete Stock Solution Preparation Table

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

A-485 Related Classifications

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.

Keywords:

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

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A-485

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A-485 Related Antibodies

53 Publications Citing Use of MCE A-485

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References

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Complete Stock Solution Preparation Table

A-485 Related Classifications

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