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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
A366
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1527503-11-2
- 规格：
50mg/25mg/1mg/10mg/5mg
| 规格： | 50mg | 产品价格： | ￥3853.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2065.0 |
| 规格： | 1mg | 产品价格： | ￥288.0 |
| 规格： | 10mg | 产品价格： | ￥969.0 |
| 规格： | 5mg | 产品价格： | ￥738.0 |
A-366是一种有效的、选择性的G9a/GLP组蛋白甲基转移酶抑制剂。
| 基本信息 | |
| CAS | No.1527503-11-2 |
| 英文名称 | A366 |
| 别名 | ;A-336;A366;A-366; |
| 分子式 | C19H27N3O2 |
| 分子量 | 329.44 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 808-907-0 |
| MDL | MFCD28133403 |
| SMILES | COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4 |
| 靶点 | Histone Methyltransferase |
| 通路 | Epigenetics |
| 背景说明 | A-366是一种有效的、选择性的G9a/GLP组蛋白甲基转移酶抑制剂。 |
| 生物活性 | A-366 is a potent， highly selective， peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1)， respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent， nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families[1-4]. |
| In Vitro | A-366(0.01-10 μM; 14 days)induces differentiation and affects viability in MV4;11 cells[4].A-366(0.3-3 μM; 72 hours)reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366(0.01-10 μM; 4 days; HL-60 cells)results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis[4]. |
| 细胞实验 | A-366(30 mg/kg; osmotic mini-pump; daily for 14 days)treatment of MV4;11 xenografts elicits growth inhibition[4]. |
| 动物实验 | Animal Model: 6-8 week old SCID-beige female mice(MV4;11 xenografts)；Dosage: 30 mg/kg；Administration: By osmotic mini-pump; daily for 14 days[4] |
| 数据来源文献 | [1]. Reiner D， et al. Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader-Willi Syndrome. Sci Rep. 2020;10(1):13558. Published 2020 Aug 11. [2]. Wagner T， et al. Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. Nucleic Acids Res. 2016;44(9):e88. [3]. Sweis RF， et al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014;5(2):205-209. Published 2014 Jan 2. [4]. Pappano WN， et al. The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia. PLoS One. 2015;10(7):e0131716. Published 2015 Jul 6. |
| 单位 | 瓶 |
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IA4090 A366 表观遗传学 索莱宝
￥288 - 3853
