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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- CAS号：
1889279-16-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3895.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1100.0 |
| 规格： | 5 mg | 产品价格： | ￥3300.0 |
| 规格： | 10 mg | 产品价格： | ￥5000.0 |
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A-485
CAS No. : 1889279-16-6
MCE 国际站：A-485
产品活性：A-485 是 p300/CBP 的强效选择性催化抑制剂，对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC50 值分别为 9.8 nM 和 2.6 nM。
研究领域：Epigenetics
作用靶点：Epigenetic Reader Domain | Histone Acetyltransferase
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.
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.
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文献和实验转录的下游调控。 1、组蛋白乙酰转移酶（HATs） 组蛋白乙酰转移酶（HATs）催化乙酰基转移 (写入) 到组蛋白尾巴上的目标赖氨酸 (Lys或K) 残基的基团上，可以中和赖氨酸的正电荷，使浓缩的染色质松弛，促进基因转录的激活，还为具有识别该组蛋白修饰的 "结合基序蛋白" (如读取蛋白 BRDs) 提供了结合位点。常用的HTAs抑制剂如下表所示： 货号 CAS 名称 特点 abs814589 1889279-16-6 A-485 p300/CBP 的强效选择性抑制剂，对 p300
3.930 4.318 13 0.694 1.350 1.771 2.160 2.650 3.012 3.372 3.852 4.221 14 0.692 1.345 1.761 2.145 2.624 2.977 3.326 3.787 4.140 15 0.691 1.341 1.753 2.131 2.602 2.947 3.286 3.733 4.073 16 0.690 1.337 1.746 2.120 2.583 2.921 3.252
,Greenberg MF.The regulation and function of c-fos and other immediate early genes in the nervous system .Neuron 1990;4:477～485 16.Francis Armstrong C,Jorgensen AO.Structure and development of E-C coupling units in skeletal muscle .Ann Rev Physiol
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