Methylstat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.

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).

Methylstat

Others

Other Targets

JMJD2A; JMJD2C; JMJD2E; PHF8; JMJD3

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1310877-95-2

505.56

C28H31N3O6

98%

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O=C(OC)/C=C/C(N(O)CCCCNCC1=CC=C(COC(NC2=C3C=CC=CC3=CC=C2)=O)C=C1)=O

(2E)-4-[Hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]-amino]butyl]amino]-4-oxo-2-butenoic acid methyl ester

(-20℃)

With Ice Pack

≥ 2 years