A-366
| 中文名称 | A-366 |
|---|---|
| 中文同义词 | G9A/GLP抑制剂(A-366);化合物A366;5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺;A 366,G9A / GLP抑制剂;5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺 |
| 英文名称 | 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine |
| 英文同义词 | 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine;A-366;A-336;CS-2077;A-366; A366;A 366;5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine;Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-;11,selective,cells,peptide-competitive,epigenetics,Inhibitor,interaction,inhibit,H3K4me3,Epigenetic Reader Domain,leukemia,Histone Methyltransferase,methyltransferase |
| CAS号 | 1527503-11-2 |
| 分子式 | C19H27N3O2 |
| 分子量 | 329.44 |
| EINECS号 | 808-907-0 |
| 相关类别 | 抑制剂;细胞生物学试剂 |
| Mol文件 | 1527503-11-2.mol |
| 结构式 |  |
A-366 性质
| 沸点 | 533.6±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.29±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：50 mg/mL（151.77 mM；需要超声波） |
| 酸度系数(pKa) | 10.18±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
A-366 是一种高效、高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC50 分别为 3.3 和 38 nM。A-366 比其他 21 种甲基转移酶具有 1000 倍以上的选择性。A-366 是一种有效的 Spindlin1-H3K4me3 相互作用的抑制剂 (IC50=182.6 nM)。A-366 对人 H3R (Ki=17 nM) 表现出很高的亲和力，并且在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。
A-366 (0.01-10 μM; 14 days) induces differentiation and affects viability in MV4;11 cells.
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.
Cell Viability Assay
| Cell Line: | MV4;11 cells |
| Concentration: | 0.01-10 μM |
| Incubation Time: | 14 days |
| Result: | Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining. |
A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.
| 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 |
| Result: | A modest 45% tumor growth inhibition resulting from A-366 treatment in this model. |
安全信息
| 危险品运输编号 | UN 3077 9 / PGIII |
|---|---|
| WGK Germany | 3 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12583 | A-366 A-366 | 1527503-11-2 | 5mg | 748元 |
| 2024/04/30 | HY-12583 | A-366 A-366 | 1527503-11-2 | 10mM * 1mLin DMSO | 825元 |