| Cat.No.: | BSM-0290 |
| Product Name: | Methylstat (hydrate) |
| Figure: |
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| Product Overview: | A cell-permeable demethylase inhibitor |
| 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). |
| Appearance: | A crystalline solid |
| Molecular Weight: | 523.6 |
| Purity: | ≥98% |
| Storage: | -20°C |
| Targets: | JMJD |
| Molecular Formula: | C28H31N3O6 • H2O |
| Chemical Name: | 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2E-butenoic acid, methyl ester, monohydrate |
| Warning: | For Research Use Only! Not For Use in Humans. |
| Product Types | ||
| ◆ Bioactive Small Molecules | ||
| BSM-0027 | UNC0321 (trifluoroacetate salt) | Inquiry |
| ◆ Antibodies | ||
| EAb-0072 | JMJD6 Polyclonal Antibody | Inquiry |
| EAb-0074 | JMJD2c Polyclonal Antibody | Inquiry |
| EAb-0075 | JMJD2b Polyclonal Antibody | Inquiry |
| EAb-0076 | JMJD2A Polyclonal Antibody | Inquiry |
| Related Gene / Proteins | |||
| JMJD | JMJD1A | JMJD1B | JMJD1C |
| JMJD2 | JMJD2A | JMJD2B | JMJD2C |
| JMJD2D | JMJD2E | JMJD2F | JMJD3 |
| JMJD4 | JMJD5 | JMJD6 | |
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