Methylstat, jumonji C domain-containing histone demethylase inhibitor (ab144566)

Overview

  • Product name
    Methylstat, jumonji C domain-containing histone demethylase inhibitor
  • Description
    Selective Jumonji C domain-containing histone demethylase inhibitor
  • Biological description
    Selective Jumonji C domain-containing histone demethylase inhibitor. Anticancer agent, inhibits esophageal carcinoma cell growth (GI50 = 5.1 μM). Cell-permeable. Active in vivo and in vitro.
  • Purity
    > 90%
  • CAS Number
    1310877-95-2
  • Chemical structure
    Chemical Structure

Properties

  • Chemical name
    (2E)-4-[Hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2-butenoic acid methyl ester
  • Molecular weight
    505.57
  • Molecular formula
    C28H31N3O6
  • Storage instructions
    Store at +4°C. It is important to note that this product is reported to be light sensitive. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview
    Soluble in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES
    O=C(OC)/C=C/C(=O)N(O)CCCCNCc1ccc(cc1)COC(=O)Nc3cccc2ccccc23
  • Source

    Synthetic

Images

  • ab9050 staining Histone H3 (tri methyl K36) in MCF-7 cells. The cells were incubated with 15µM Methylstat (ab144566) for 24 hours (Treated) or solvent-only for control purposes (Non-treated). Cells were fixed with 100% methanol (5min) and then blocked in 1% BSA/10% normal goat serum/0.3M glycine in 0.1%PBS-Tween for 1h. The cells were then incubated with ab9050 at 0.1µg/ml and ab195889 Mouse monoclonal [DM1A] to alpha Tubulin - Alexa Fluor® 594 at 2µg/ml (shown in pseudo colour red) overnight at +4°C, followed by a further incubation at room temperature for 1h with an AlexaFluor®488 Goat anti-Rabbit secondary (ab150081) at 1/1000 dilution (shown in green). Nuclear DNA was labelled in blue with DAPI. Negative controls: 1– anti-rabbit secondary only (solvent only); 2 – anti-rabbit secondary only (Treated). The secondary antibody control demonstrates that the labelling observed is due only to the binding of the secondary antibody to the primary antibody

References

This product has been referenced in:
  • Xu W  et al. Quantitative analysis of histone demethylase probes using fluorescence polarization. J Med Chem 56:5198-202 (2013). Read more (PubMed: 23725560) »
  • Luo X  et al. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. J Am Chem Soc 133:9451-6 (2011). Read more (PubMed: 21585201) »

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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