Epigenetics

Methylstat View larger

Methylstat

AT7057

CAS 1310877-95-2

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$169.00

$169.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
1100 $76.05 Total: $7,605.00
150 $87.88 Total: $4,394.00
125 $103.09 Total: $2,577.25
110 $121.68 Total: $1,216.80
15 $143.65 Total: $718.25

Data sheet

Molecular FormulaC28H31N3O6
Molecular Weight505.56
CAS Numbers1310877-95-2
Storage Condition0C Short Term, -20C Long Term
SolubilityDMSO
Purity98% by HPLC
SMILES CodeCOC(=O)C=CC(=O)N(O)CCCCNCc1ccc(COC(=O)Nc2cccc3ccccc23)cc1
ReferencesLuo, X., et al. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. Journal of the American Chemical Society 133[24], 9451-9456 [2011].

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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 ?M, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 ?M, whereas the free acid of methylstat did not inhibit cell growth up to 100 ?M. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 ?M in KYSE150 cells and 6.7 ad 6.3 ?M in MCF-7 cells, respectively).