AA-BR-157
Based on 1 Customer Validation
AA-BR-157 is a metallothionein 2A (MT2A) PROTAC degrader, DC50 is 200 nM (MT2A overexpressed in MDA-MB-231 cells). AA-BR-157 increases intracellular zinc levels, downregulates DIAPH3, disrupts cytoskeleton remodeling, and reduces the migration and invasion abilities of cancer cells. AA-BR-157 can be used for research on triple-negative breast cancer and glioblastoma.
(Pink: MT2A ligand (HY-168970); Blue: VHL ligand (HY-125845); Black: linker (HY-119429)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 96.47%
- 分子式: C56H70N8O11S2
- 分子量:1095.33
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
AA-BR-157 (0-30 μM; 24 h) (Compound 17) potently degrades overexpressed MT2A in MDA-MB-231 cells, with a DC50 of 200 nM and a Dmax of 90%[1].
AA-BR-157 (0-10 μM; 24 h) inhibits the migration of MDA-MB-231 and U-87 MG cells, as well as the invasion of MDA-MB-231 cells[1].
AA-BR-157 (10 μM; 12-24 h) increases intracellular zinc levels in MDA-MB-231 cells[1].
AA-BR-157 (0-10 μM; 24 h) downregulates the expression of DIAPH3 in MDA-MB-231 cells[1].
AA-BR-157 (10 μM; 24 h) induces a non-polarized, non-migratory cytoskeletal morphology in MDA-MB-231 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:stable MT2A-V5 overexpressing MDA-MB-231 (MT2A OE) cells
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Concentration:0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30 μM (24 h incubation); 10 μM (time-course analysis)
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Incubation Time:24 h (dose-dependent assay); varying times (time-course analysis)
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Result:Induced a dose-dependent decrease in MT2A levels, with a half-maximal degradation concentration (DC50) of 200 nM and a maximal degradation (Dₘₐₓ) of 90% starting at ~1 μM.
Showed no protein recovery at higher concentrations, indicating no Hook effect.
Revealed a half-maximal degradation time (D50) of 14.6 h, with maximum degradation achieved after 24 h.
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Cell Line:MDA-MB-231 cells, U-87 MG cells
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Concentration:0, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Caused a concentration-dependent decrease in cellular migration, with a maximal decrease of greater than 60% at 10 μM in both MDA-MB-231 and U-87 MG cells, matching the effect of MT siRNA knockdown.
Inhibited MDA-MB-231 cell invasion through Matrigel at 10 μM.
Showed no cell death in a WST-1 assay, confirming the effects were not due to cytotoxicity.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 3, 10 μM
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Incubation Time:24 h
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Result:Downregulated DIAPH3 with a ratio of 0.31 for AA-BR-157/DMSO in global proteomics analysis, matching the effect of MT siRNA knockdown.
Confirmed an ~50% decrease in DIAPH3 levels following treatment with 10 μM AA-BR-157 via Western blot, mirroring the effect of MT siRNA.
化学情報
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性状 Solid
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分子量 1095.33
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分子式 C56H70N8O11S2
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Color White to off-white
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SMILES
O=C(NCC1=NC2=CC(C3=CC=CC(C(N4CCN(C(C=C)=O)CC4)=O)=C3)=CC=C2S1)CCOCCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (91.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9130 mL | 4.5648 mL | 9.1297 mL | 22.8242 mL |
| 5 mM | 0.1826 mL | 0.9130 mL | 1.8259 mL | 4.5648 mL | |
| 10 mM | 0.0913 mL | 0.4565 mL | 0.9130 mL | 2.2824 mL | |
| 15 mM | 0.0609 mL | 0.3043 mL | 0.6086 mL | 1.5216 mL | |
| 20 mM | 0.0456 mL | 0.2282 mL | 0.4565 mL | 1.1412 mL | |
| 25 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9130 mL | |
| 30 mM | 0.0304 mL | 0.1522 mL | 0.3043 mL | 0.7608 mL | |
| 40 mM | 0.0228 mL | 0.1141 mL | 0.2282 mL | 0.5706 mL | |
| 50 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.4565 mL | |
| 60 mM | 0.0152 mL | 0.0761 mL | 0.1522 mL | 0.3804 mL | |
| 80 mM | 0.0114 mL | 0.0571 mL | 0.1141 mL | 0.2853 mL |
AA-BR-157 関連分類
HY-168969 関連分類
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