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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-A-485
A-485

Chemical Structure : A-485

CAS No.: 1889279-16-6

A-485 (A485;A 485)

货号: PC-60028Not For Human Use, Lab Use Only.

A-485 (A485) is a potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

A-485 (A485) is a potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.
A-485 displays selectivity for p300/CBP over other HATs and histone methyltransferases in cells.
A-485 dose-dependently decreases H3K27Ac in prostate adenocarcinoma PC-3 cells with EC50 of 73 nM.
A-485 selectively inhibits proliferation in lineage-specific tumour types.
A-485 inhibits the AR transcriptional program in both androgen-sensitive and castration-resistant prostate cancer and inhibits tumour growth in a castration-resistant xenograft model.

物理化学性质&存储条件

分子量 536.484
分子式 C25H24F4N4O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-fluorobenzyl)-2-((R)-5-(3-methylureido)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-3'-yl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide

参考文献

1. Lasko LM, et al. Nature. 2017 Oct 5;550(7674):128-132.

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