Methylstat
Catalog No. T7057 CAS
1310877-95-2
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).
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Methylstat, CAS 1310877-95-2
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description |
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). |
Targets&IC50 |
JMJD2A:4.3 µM, PHF8:10 µM , JMJD2E:5.9 µM, JMJD3:43 µM, JMJD2C:3.4 µM
|
Molecular Weight |
505.571
|
Formula |
C28H31N3O6 |
CAS No. |
1310877-95-2 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 25 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
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Keywords
Methylstat
1310877-95-2
表观遗传
其他
Histone Demethylase
Others
anti-proliferative
HUVECs
anti-angiogenic
G0/G1 phase
Apoptosis
p53
Inhibitor
MDM-2/p53
low cytotoxicity
inhibit
inhibitor