| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D409211-1ml |
1ml |
现货  |
|
| 别名 | 达西司他 (LAQ824) |
|---|---|
| 英文别名 | NVP-LAQ824 | (E)-3-(4-(((2-(1H-indol-3-yl)ethyl)(2-hydroxyethyl)amino)methyl)phenyl)-N-hydroxyacrylamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Dacinostat (LAQ824) |
| 生化机理 | 达西诺司他（LAQ824，NVP-LAQ824）是一种新型 HDAC 抑制剂，其 IC50 值为 32 nM，可激活 p21 启动子。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 组蛋白去乙酰化酶 1 抑制剂；组蛋白去乙酰化酶 2 抑制剂；组蛋白去乙酰化酶 3 抑制剂；组蛋白去乙酰化酶 4 抑制剂；组蛋白去乙酰化酶 5 抑制剂；组蛋白去乙酰化酶 6 抑制剂；组蛋白去乙酰化酶 7 抑制剂；组蛋白去乙酰化酶 8 抑制剂；组蛋白去乙酰化酶 9 抑制剂 |
| 产品介绍 |
LAQ824（NVP-LAQ824）是一种新型HDAC抑制剂，IC | 50 |为32 nM。LAQ824以0.30μM的最大启动子激活（AC | 50 |）的50％激活p21启动子，从而激活p21抑制剂基因。LAQ824抑制IC50分别为0.15μM和0.01μM的H1299（非小细胞肺癌细胞系）和HCT116（结肠癌细胞系）的细胞生长。最近的一项研究表明，LAQ824会在IL-10基因启动子水平上诱导染色质变化，从而导致转录阻遏物HDAC11和PU.1的募集增加，并抑制BALB / c鼠巨噬细胞中IL 应用： Dacinostat 是一种有效的 HDAC 抑制剂，IC50 值为 32 nM；Dacinostat 同时可抑制 HDAC1 的活性，IC50 值为 9 nM，主要用于癌症研究。 Information Dacinostat (LAQ824) Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter. LAQ824 activates the expression of the gene encoding the p21 cell cycle inhibitor by activating the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM. LAQ824 inhibits the cell growth of both H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively, and the antiproliferative effect of LAQ824 is selective toward the tumor cell lines while inducing only growth arrest in normal fibroblasts. Furthermore, LAQ824 induces a dose-dependent increase of p21 protein in A549 cells and an increase in the hypophosphorylated state of the Rb tumor suppressor. A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages. In vivo In HCT116 and human colon tumor xenografts in nude mice, LAQ824 treatment at 100 mg/kg produces the inhibitory effects on tumor growth in a dose-dependent mode without general cytotoxicity. cell lines： Concentrations：0-10 μM Incubation Time：48 hours Powder Purity:≥95% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)/C=C/C(=O)NO |
| 分子量 | 379.45 |
| Reaxy-Rn | 18447870 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18447870&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 29 mg/mL (20.01 mM); Water: Insoluble; Ethanol: Insoluble; |
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