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Methylstat

CAT: 0931-T7057Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0931-T7057Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1310877-95-2
Target
Apoptosis, Histone Demethylase, MDM-2/p53
Related Pathways
Apoptosis, Chromatin/Epigenetic
Purity
0.9834
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) .
Smiles
COC(=O)\C=C\C(=O)N(O)CCCCNCc1ccc(COC(=O)Nc2cccc3ccccc23)cc1
Molecular Formula
C28H31N3O6
Molecular Weight
505.56
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

Alternative Products

CatalogName
M19349-01Methylstat
B2836-5Methylstat (hydrate)
KCC87795-01JMJD Histone Demethylase Inhibitor IV, Methylstat
217483JMJD Histone Demethylase Inhibitor IV, Methylstat ((E) -Methyl-4- (hydroxy (4- ((4- (((naphthalen-1-ylcarbamoyl) oxy) methyl) benzyl) amino) butyl) amino) -4-oxobut-2-enoate, Histone Lysine Demethylase Inhibitor VII, Methylstat)

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