| Identification | Back Directory | [Name]
METHYLSTAT | [CAS]
1310877-95-2 | [Synonyms]
METHYLSTAT
Methylstat >=98% (HPLC)
MUJOCHRZXRZONW-FOCLMDBBSA-N
JMJD Histone Demethylase Inhibitor IV, Methylstat
JMJD Histone Demethylase Inhibitor IV, Methylstat - CAS 1310877-95-2 - Calbiochem
(E)-methyl 4-(N-hydroxy-4-(4-((naphthalen-1-yl-carbamoyloxy)methyl)benzylamino)butylamino)-4-oxobut-2-enoate
(2E)-4-[Hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-2-butenoic acid methyl ester
2-Butenoic acid, 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-, methyl ester, (2E)- | [Molecular Formula]
C28H31N3O6 | [MDL Number]
MFCD22572723 | [MOL File]
1310877-95-2.mol | [Molecular Weight]
505.56 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: >5mg/mL | [form ]
powder | [color ]
white to beige | [InChIKey]
MUJOCHRZXRZONW-FOCLMDBBSA-N | [SMILES]
O=C(NC1=CC=CC2=C1C=CC=C2)OCC3=CC=C(CNCCCCN(O)C(/C=C/C(OC)=O)=O)C=C3 |
| Hazard Information | Back Directory | [Uses]
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis[1][2]. | [Definition]
ChEBI: 4-[hydroxy-[4-[[4-[[(1-naphthalenylamino)-oxomethoxy]methyl]phenyl]methylamino]butyl]amino]-4-oxo-2-butenoic acid methyl ester is a member of naphthalenes. | [Biological Activity]
Methylst at is an inhibitor of the Jumonji C domain-containing histone trimethyl demethylases (JHDMs). Methylst at inhibits the activity of JMJD2C (IC50 = 4.3 μM), with similar potency against JMJD2E and JMJD3. The compound has poor activity against dimethyl demethylases, and does not inhibit class I or II HDACs. Methyls at blocks proliferation of the esophageal carcinoma cell line KYSE150 with an IC50 value of 5.1 μM. | [References]
[1] Yumi Cho, et al. A histone demethylase inhibitor, methylstat, inhibits angiogenesis in vitro and in vivo. RSC Advances, 2014.
[2] Kac? FN, et al. Synergistic Apoptotic Effects of Bortezomib and Methylstat on Multiple Myeloma Cells. Arch Med Res. 2020 Apr;51(3):187-193. DOI:10.1016/j.arcmed.2020.01.012 |
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Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
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21-20338288 |
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www.sigmaaldrich.cn |
| Company Name: |
Abcam Limited
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021-2070050 400921018 |
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www.abcam.cn |
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