SR-0813

CAS No. 2597186-19-9

SR-0813( —— )

Catalog No. M35189 CAS No. 2597186-19-9

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    SR-0813
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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.
  • 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.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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Chromatin/Epigenetic
  • Target
    Epigenetic Reader Domain
  • Recptor
    Epigenetic Reader Domain
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2597186-19-9
  • Formula Weight
    496.62
  • Molecular Formula
    C25H32N6O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (201.36 mM; Ultrasonic )
  • SMILES
    C(NC1CCC1)(=O)C2=CN3C(=NC(=C3)C4=CC(NS(NCCN5CCCCC5)(=O)=O)=CC=C4)C=C2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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