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Submit ReviewAMZ 30 is a potent, selective and irreversible inhibitor of protein phosphatase methylesterase-1 (PME-1; IC50 = 600 nM) with > 100-fold selectivity for PME-1 over other serine hydrolases in human cell lysates. AMZ 30 inactivates PME-1 and reduces the demethylated form of serine/threonine protein phosphatase 2A (PP2A) in HEK 293T cells. AMZ 30 perturbs leucine carboxyl methyltransferase-1 (LCMT1)-PME-1 methylation equilibrium leading to shortening of mitotic spindles and mitotic arrest in HeLa cells. It also shows antiproliferative properties in an in vitro model of endometrial carcinoma.
分子量 | 461.45 |
公式 | C19H12FN3O6S2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1313613-09-0 |
PubChem ID | 44607965 |
InChI Key | GUCUORSUHTZMBW-YBFXNURJSA-N |
Smiles | C(=C(/S(=O)(=O)C1=CC=C(F)C=C1)\C#N)\C=2N(S(=O)(=O)C3=CC(N(=O)=O)=CC=C3)C=CC2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.15 | 100 |
以下数据基于产品分子量 461.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.17 mL | 10.84 mL | 21.67 mL |
5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Elgenaidi et al (2019) Regulation of the phosphoprotein phosphatase 2A system and its modulation during oxidative stress: A potential therapeutic target? Pharmacol.Ther. 198 68 PMID: 30797822
Xia et al (2015) A LCMT1-PME-1 methylation equilibrium controls mitotic spindle size. Cell Cycle 14 1938 PMID: 25839665
Bachovchin et al (2011) Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J.Med.Chem. 54 5229 PMID: 21639134
If you know of a relevant reference for AMZ 30, please let us know.
关键词: AMZ 30, AMZ 30 supplier, AMZ30, potent, selective, irreversible, covalent, inhibitor, inhibits, serine, hydrolases, protein, phosphatase, methylesterase-1, PME-1, mitotic, arrest, Other, Hydrolases, Mitosis, 6923, Tocris Bioscience
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