1310877-95-2
1310877-95-2 structure
- Name: Methylstat
- Chemical Name: Methyl (2E)-4-(hydroxy{4-[(4-{[(1-naphthylcarbamoyl)oxy]methyl}benzyl)amino]butyl}amino)-4-oxo-2-butenoate
- CAS Number: 1310877-95-2
- Molecular Formula: C28H31N3O6
- Molecular Weight: 505.562
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-06-19 14:12:55
- Modify Date: 2025-08-25 13:10:42
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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].
| Name | Methyl (2E)-4-(hydroxy{4-[(4-{[(1-naphthylcarbamoyl)oxy]methyl}benzyl)amino]butyl}amino)-4-oxo-2-butenoate |
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| Synonyms |
2-Butenoic acid, 4-[hydroxy[4-[[[4-[[[(1-naphthalenylamino)carbonyl]oxy]methyl]phenyl]methyl]amino]butyl]amino]-4-oxo-, methyl ester, (2E)-
4-[hydroxy-[4-[[4-[[(1-naphthalenylamino)-oxomethoxy]methyl]phenyl]methylamino]butyl]amino]-4-oxo-2-butenoic acid methyl ester Methyl (2E)-4-(hydroxy{4-[(4-{[(1-naphthylcarbamoyl)oxy]methyl}benzyl)amino]butyl}amino)-4-oxo-2-butenoate |
| Description | 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]. |
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| Related Catalog | |
| In Vitro | Methylstat (0-5 µM; 48, 72 h) shows anti-proliferative activity with no cytotoxicity on HUVECs at 1-2 µM[1]. Methylstat (0, 1, 2 µM; 48 h) induces cell cycle arrest at G0/G1 phase in a dose-dependent manner[1]. Methylstat (0, 1, 2 µM; 48 h) increases the expression of p53 mRNA levels, the H3K27 methylation levels and the accumulation of p53 and p21 protein levels, but suppresses the protein level of cyclinD1[1]. Methylstat (0, 1, 2 µM) shows anti-angiogenic activity induced by VEGF, bFGF and TNF-α in HUVEC cells, and inhibits the f capillary formation during CAM (chick embryo chorioallantoic membrane) development without any sign of thrombosis and hemorrhage[1]. Methylstat (1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells; 72 h) induces apoptosis significantly in U266 and ARH77 cells[2]. Cell Cytotoxicity Assay[1] Cell Line: HUVEC cells Concentration: 0-5 µM Incubation Time: 48, 72 h Result: Did not exhibit cytotoxicity on HUVECs at 1-2 µM. Cell Viability Assay[1] Cell Line: HUVEC, HepG2, HeLa, CHANG cells Concentration: 0-5 µM Incubation Time: 72 h Result: Showed anti-proliferative activity with IC50s of 4, 10, 5, 7.5 µM for HUVEC, HepG2, HeLa, CHANG cells, respectively. Cell Cycle Analysis[1] Cell Line: HUVEC cells Concentration: 0, 1, 2 µM Incubation Time: 48 h Result: G0/G1 phase increased 16.8% compared to non-treated cells, whereas S andG2/M decreased 5.5% and 6.1% respectively. Western Blot Analysis[1] Cell Line: HUVEC cells Concentration: 0, 1, 2 µM Incubation Time: 0-48 h Result: Resulted in accumulation of p53 and p21 protein levels in a time- and dose-dependent manner and increased the H3K27 methylation levels, the but suppressed the protein level of cyclinD1. Apoptosis Analysis[2] Cell Line: U266, ARH77 cells Concentration: 1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells Incubation Time: 72 h Result: Induced apoptosis in U266, ARH77 cells. |
| References |
| Density | 1.3±0.1 g/cm3 |
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| Molecular Formula | C28H31N3O6 |
| Molecular Weight | 505.562 |
| Exact Mass | 505.221283 |
| LogP | 3.30 |
| Index of Refraction | 1.635 |
| RIDADR | NONH for all modes of transport |
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