SR-0813

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

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.

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Chromatin/Epigenetic

Epigenetic Reader Domain

Epigenetic Reader Domain

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2597186-19-9

496.62

C25H32N6O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (201.36 mM; 超声助溶 )

C(NC1CCC1)(=O)C2=CN3C(=NC(=C3)C4=CC(NS(NCCN5CCCCC5)(=O)=O)=CC=C4)C=C2

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(-20℃)

With Ice Pack

≥ 2 years