Methylstat

CAS No. 1310877-95-2

Methylstat ( Methylstat )

Catalog No. M19349 CAS No. 1310877-95-2

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.

Purity : 98%

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Methylstat
  • Note
    Research use only, not for human use.
  • Brief Description
    Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.
  • Description
    Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).
  • Synonyms
    Methylstat
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    JMJD2A; JMJD2C; JMJD2E; PHF8; JMJD3
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1310877-95-2
  • Formula Weight
    505.56
  • Molecular Formula
    C28H31N3O6
  • Purity
    98%
  • Solubility
    ——
  • SMILES
    O=C(OC)/C=C/C(N(O)CCCCNCC1=CC=C(COC(NC2=C3C=CC=CC3=CC=C2)=O)C=C1)=O
  • Chemical Name
    (2E)-4-[Hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]-amino]butyl]amino]-4-oxo-2-butenoic acid methyl ester

Shipping & Storage Information

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

Reference

1. Luo, X., et al. Journal of the American Chemical Society 133(24), 9451-9456 (2011).
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