AMZ 30

Pricing Availability   Qty
说明: Potent, selective and irreversible protein phosphatase methylesterase-1 (PME-1) inhibitor
化学名: (2E)-2-[(4-Fluorophenyl)sulfonyl]-3-[1-[(3-nitrophenyl)sulfonyl]-1H-pyrrol-2-yl]-2-propenenitrile
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for AMZ 30

AMZ 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.

技术数据 for AMZ 30

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.

溶解性数据 for AMZ 30

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.15 100

制备储备液 for AMZ 30

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for AMZ 30

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


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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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