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 IC 50 and EC 50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC 50 and EC 50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity ( K d =3.5 μM) than ENL YEATS ( K d =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 [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] . 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.

2597186-19-9

C25H32N6O3S

496.63

(< 1 mg/ml refers to the product slightly soluble or insoluble )
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