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A-485

Catalog No. T14073   CAS 1889279-16-6

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

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A-485 Chemical Structure
A-485, CAS 1889279-16-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 89.00
2 mg In stock $ 123.00
5 mg In stock $ 179.00
10 mg In stock $ 320.00
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1 mL * 10 mM (in DMSO) In stock $ 219.00
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Purity: 100%
Purity: 98.32%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A-485 is a potent and selective catalytic p300/CBP inhibitor(IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively).
Targets&IC50 p300:9.8 nM, CBP:2.6 nM
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. 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. Treatment with A-485 does not alter p300 or CBP protein levels, but it induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines[1].
In vivo A-485, a potent, selective and drug-like catalytic inhibitor of p300 and CBP.?A-485 selectively inhibited proliferation in lineage-specific tumour types, including several haematological malignancies and androgen receptor-positive prostate cancer.?A-485 inhibited the androgen receptor transcriptional program in both androgen-sensitive and castration-resistant prostate cancer and inhibited tumour growth in a castration-resistant xenograft model.?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).?A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen[1].?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.?But, 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.
Molecular Weight 536.48
Formula C25H24F4N4O5
CAS No. 1889279-16-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (186.40 mM), sonification is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
PPI Inhibitor Library Anti-Hypertension Compound Library Reprogramming Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library Epigenetics Compound Library Histone Modification Compound Library Stem Cell Differentiation Compound Library Inhibitor Library

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Keywords

A-485 1889279-16-6 Chromatin/Epigenetic Histone Acetyltransferase Epigenetic Reader Domain inhibit HATs Inhibitor A485 HAT A 485 inhibitor

 

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