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Methylstat

Chemical Structure : Methylstat

CAS No.: 1310877-95-2

Methylstat

Catalog No.: PC-25582Not For Human Use, Lab Use Only.

Methylstat is a selective inhibitor of Jumonji C domain-containing histone demethylases (JHDMs) in cells, preferentially inhibits JMJD2A (H3K9me3 and H3K36me3 demethylase), JMJD2E (H3K9me3 demethylase) and JMJD3 (H3K27me3 demethylase).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Methylstat is a selective inhibitor of Jumonji C domain-containing histone demethylases (JHDMs) in cells, preferentially inhibits JMJD2A (H3K9me3 and H3K36me3 demethylase), JMJD2E (H3K9me3 demethylase) and JMJD3 (H3K27me3 demethylase).
Methylstat does not inhibit class I or class II HDACs, FAD-dependent demethylase LSD1, and weak activity against α-ketoglutarate-dependent hydroxylases such as prolyl hydroxylases PHD1-3.
Methylstat inhibited KYSE150 cell growth with IC50 of 5.1 uM.
Methylstat increased cellular levels of both H3K4me3 and H3K9me3 in KYSE150 cells with EC50 of 10.3 μM and 8.6 μM, respectively.
Methylstat (1-4 uM) prevents myogenesis through inhibition of H3K27me3-demethylase UTX in C2C12 cells.

Physicochemical Properties

M.Wt 505.57
Formula C28H31N3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Butenoic acid, 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-, methyl ester, (2E)-

References

1. Luo X, et al. J Am Chem Soc. 2011 Jun 22;133(24):9451-6.

2. Yao H, et al. Pharmaceuticals (Basel). 2025 Sep 8;18(9):1344.

3. Schwarz FM, et al. Cancer Gene Ther. 2025 Mar;32(3):286-296.

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