GSK-J4 (hydrochloride)
货号：
12073-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 12073-1mg |
| 描述 | The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.1,2 GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.3 Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Agger, K.,Cloos, P.A.C.,Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development. Nat.Lett. 449(7163), 731-734 (2011).
2.Hübner, M.R., and Spector, D.L. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation. Cold Spring Harb.Symp.Quant.Biol. 75, 43-49 (2010).
3.Kruidenier, L.,Chung, C.W.,Cheng, Z., et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488, 404-408 (2012).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 454 |
| 分子式 | C24H27N5O2 • HCl |
| CAS号 | 1797983-09-5 |
| 稳定性 | ≥ 2 years |
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