货号	规格	价格	上海	北京	珠海	重庆	武汉
S89129-5mg	98.00%	￥300.00 S89129-5mg ￥300.00 现货	2 2	-	-	-	-
S89129-10mg	98.00%	￥540.00 S89129-10mg ￥540.00 现货	5 5	-	-	-	-
S89129-25mg	98.00%	￥1050.00 S89129-25mg ￥1050.00 现货	2 2	-	-	-	-
S89129-100mg	≥98%	￥3720.00 S89129-100mg ￥3720.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels

靶点：

KDM5 histone demethylase;HistoneDemethylase

体外研究：

KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM). KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression. Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay Cell Line: MM.1S myeloma cells Concentration: 10-9-10-5 M Incubation Time: 7 days Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations. Western Blot Analysis Cell Line: MM.1S myeloma cells Concentration: 50 μM Incubation Time: 7 days Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb).

参考文献：

1. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45. 2. Blair LP, et al. KDM5 lysine demethylases are involved in maintenance of 3'UTR length. Sci Adv. 2016 Nov 18;2(11):e1501662.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.972 ml	14.862 ml	29.723 ml
5 mM	0.594 ml	2.972 ml	5.945 ml
10 mM	0.297 ml	1.486 ml	2.972 ml
50 mM	0.059 ml	0.297 ml	0.594 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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