AM 114 (Synonyms: PS-IX; AM114) |
カタログ番号GC13789 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 856849-35-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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。
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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