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Methylstat (hydrate)

A prodrug of a Jumonji C domain-containing histone demethylase (JMJD)
Catalog #: B2836
SKU-Size Size Price Qty
B2836-1 1 mg
$85.00
B2836-5 5 mg
$295.00
More Sizes Get Quote

Product Details

Alternate Name 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2E-butenoic acid, methyl ester, monohydrate; (E)-methyl 4-(hydroxy(4-((4-(((naphthalen-1-ylcarbamoyl)oxy)methyl)benzyl)amino)butyl)amino)-4-oxobut-2-enoate hydrate; Histone Lysine Demethylase Inhibitor VII; JHDM Inhibitor IV
Appearance Crystalline solid
CAS # n/a
Molecular Formula C₂₈H₃₁N₃O₆.H₂O
Molecular Weight 523.58
Purity ≥98%
Solubility ~25 mg/ml in DMSO and DMF
SMILES O=C(OC)/C=C/C(N(O)CCCCNCC1=CC=C(COC(NC2=C3C=CC=CC3=CC=C2)=O)C=C1)=O.[H]O[H]
InChi InChI=1S/C28H31N3O6.H2O/c1-36-27(33)16-15-26(32)31(35)18-5-4-17-29-19-21-11-13-22(14-12-21)20-37-28(34)30-25-10-6-8-23-7-2-3-9-24(23)25;/h2-3,6-16,29,35H,4-5,17-20H2,1H3,(H,30,34);1H2/b16-15+;
InChi Key GLUJKORUIWJKCZ-GEEYTBSJSA-N
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20ºC
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

Methylstat is a methyl ester prodrug that inhibits Jumonji C domain-containing histone demethylase (JMJD) in cells. Methylstat inhibits growth of JMJD2C-sensitive oesophageal carcinoma cell line KYSE150 cells with an IC₅₀ of approximately 5.1 μM, whereas the free acid of methylstat does not inhibit cell growth up to 100 µM. Methylstat induces hypermethylation, inhibits JMJD2C and recovers H3K9me3 levels in HeLa cells.


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