SP2509
货号：
15487-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 15487-1mg |
| 描述 | Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4), resulting in transcriptional repression.1 SP2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM).2 It has no effect on monoamine oxidases A and B. SP2509 attenuates the binding of LSD1 to CoREST, allowing increased methylation of H3K4 and driving increased expression of p21, p27, and CCAAT/enhancer binding protein α in cultured acute myeloid leukemia (AML) cells.2,3 It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks.2 Co-treatment of SP2509 with the pan-HDAC inhibitor panobinostat (Item No. 13280) synergistically kills AML cells in vitro and improves survival of mice engrafted with AML cells.2,3 |
| 别名 | HCI-2509;LSD1 Inhibitor VII; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Forneris, F.,Binda, C.,Vanoni, M.A., et al. Human histone demethylase LSD1 reads the histone code. The Journal of Biological Chemisty 280(50), 41360-41365 (2005).
2.Fiskus, W.,Sharma, S.,Abhyankar, S., et al. Pre-clinical efficacy of combined therapy with LSD1 antagonist SP-2509 and pan-histone deacetylase inhibitor against AML blast progenitor cells. 1-1.
3.Fiskus, W.,Sharma, S.,Shah, B., et al. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia 28(11), 2155-2164 (2014).
|
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 437.9 |
| 分子式 | C19H20ClN3O5S |
| CAS号 | 1423715-09-6 |
| 稳定性 | ≥ 2 years |
声明| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |
