SR-0813

Research use only, not for human use.

SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9, with an IC50 of 25 nM and EC50 of 205 nM for the ENL YEATS domain, and an IC50 of 311 nM and EC50 of 76 nM (CETSA) for the AF9 YEATS domain.

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 : 100 mg/mL (201.36 mM; Ultrasonic )

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