SR-0813

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SR-0813 

SR-0813 是一种有效的选择性 ENL/AF9 YEATS 结构域抑制剂。SR-0813 对于 ENL YEATS 结构域的 IC50 和 EC50 值分别为 25 nM 和 205 nM。SR-0813 对于 AF9 YEATS 结构域的 IC50 和 EC50 值分别为 311 nM 和 76 nM (CETSA)。SR-0813 结合 MAP3K19 的亲和力 (Kd=3.5 μM) 比 ENL YEATS (Kd=30 nM) 低 100 倍以上。SR-0813 可用于急性白血病的研究。

SR-0813

SR-0813 Chemical Structure

CAS No. : 2597186-19-9

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生物活性

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[1].

IC50 & Target[1]

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)

体外研究
(In Vitro)

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[1].
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[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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.

分子量

496.62

Formula

C25H32N6O3S
CAS 号

2597186-19-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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