货号	规格	价格	上海	北京	珠海	重庆	武汉
S89717-5mg买3赠1	99.50%	￥790.00 S89717-5mg ￥790.00 现货（买3赠1）	6 6	-	-	-	-
S89717-10mg促销	99.50%	￥1290.00 ￥1030.00 S89717-10mg ￥1030.00 现货	6 6	-	-	-	-
S89717-25mg促销	99.50%	￥2230.00 ￥1780.00 S89717-25mg ￥1780.00 现货	2 2	-	-	-	-
S89717-100mg促销	≥98%	￥4360.00 ￥3480.00 S89717-100mg ￥3480.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia

靶点：

ENL YEATS domain:25 nM (IC50);ENL YEATS domain:205 nM (EC50);AF9 YEATS domain:311 nM (IC50);AF9 YEATS domain:76 nM (EC50);ENL YEATS domain:30 nM (Kd);MAP3K19:3.5 μM (Kd);EpigeneticReaderDomain

体外研究：

SR-0813 (compound 10; 0, 1, 10 μM; 4 h) dose-dependent evicts ENL from known ENL binding sites, including the HOXA10 gene body and MYB promoter in MV4;11 cells. SR-0813 (0, 1, 10 μM; 0, 24, 48, 72 h) downregulates the transcript levels of HOXA9, MEIS1, and MYC, and increases the abundance of the ITGAM transcript in MV4;11 cells. SR-0813 (0, 1, 10 μM; approximately 2 weeks) inhibits the growth of multiple lineage leukemia (MLL)-fusion leukemia cell lines (MV4;11, MOLM-13, OCI/AML-2) and HB11;19 cells. SR-0813 (1 μM, 4h) does not elicit global changes in gene expression in MV4;11 cells, but produces a strikingly selective suppression of ENL target genes Cell Proliferation Assay Cell Line: MLL-fusion leukemia cell lines: MV4;11 (MLL-AF4 AML), MOLM-13 (MLL-AF9 AML), and OCI/AML-2 (MLL-AF6 AML), which are sensitive to the genetic loss of ENL.HB11;19 cells, which harboring an MLL-ENL fusion. Concentration: 0, 1, 10 μM Incubation Time: Approximately 2 weeks Result: Inhibited the growth of cells.

参考文献：

1. Garnar-Wortzel L, et al. Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia. ACS Cent Sci. 2021 May 26;7(5):815-830.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.014 ml	10.068 ml	20.136 ml
5 mM	0.403 ml	2.014 ml	4.027 ml
10 mM	0.201 ml	1.007 ml	2.014 ml
50 mM	0.04 ml	0.201 ml	0.403 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。

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