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AM 114 (Synonyms: PS-IX; AM114)

カタログ番号GC13789

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AM 114 化学構造

Cas No.: 856849-35-9

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10mg
$90.00
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50mg
$315.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AM 114は、ボロン酸コンジュゲートのカルコン誘導体であり、プロテアソームの強力な小分子阻害剤である。20Sプロテアソームのキモトリプシン様活性を抑制し、50%阻害濃度IC50が約1μMであるため、細胞全体においてp53や他の細胞内タンパク質がユビキチン化された状態で蓄積することが示されています。また、p53とマウスダブルミニット2(mdm2)タンパク質間の相互作用を著しく妨げることなく、癌細胞に対しても抗癌活性を示します。特に人間大腸癌HCT116細胞株に対してはMTT試験および集落形成試験においてそれぞれIC50値が1.5μMおよび0.6μMであり、強力な増殖抑制効果を有します。

参考文献

[1].Achanta G、Modzelewska A、Feng L、Khan SR、Huang P。ボロン-カルコン誘導体はプロテアソームの阻害を通じて強力な抗がん活性を示す。Mol Pharmacol. 2006年7月;70(1):426-33.オンラインで2006年4月24日に発行。

Chemical Properties

Cas No. 856849-35-9 SDF
同義語 PS-IX; AM114
Chemical Name [4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
Canonical SMILES B(C1=CC=C(C=C1)C=C2CN(CC(=CC3=CC=C(C=C3)B(O)O)C2=O)C)(O)O
Formula C20H21B2NO5 M.Wt 377.01
溶解度 ≥ 16.65mg/mL in DMSO, ≥ 4.11 mg/mL in EtOH with ultrasonic Storage Store at 4°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6524 mL 13.2622 mL 26.5245 mL
5 mM 0.5305 mL 2.6524 mL 5.3049 mL
10 mM 0.2652 mL 1.3262 mL 2.6524 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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