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)).
For research use only. We do not sell to patients.
- Purity: 96.47%
- Formula: C56H70N8O11S2
- Molecular Weight:1095.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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.
Chemical Information
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Appearance Solid
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Molecular Weight 1095.33
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
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