TargetMol

Methylstat

Product Code:
 
TAR-T7057
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T7057-5mg5mg£136.00
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Further Information

Bioactivity:
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).
CAS:
1310877-95-2
Formula:
C28H31N3O6
Molecular Weight:
505.571
Pathway:
; Chromatin/Epigenetic
Purity:
0.98
SMILES:
COC(=O)C=CC(=O)N(O)CCCCNCc1ccc(COC(=O)Nc2cccc3ccccc23)cc1
Target:
Histone Demethylase;

References

Luo, 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).