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)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 96.47%
- 화학식: C56H70N8O11S2
- 분자량:1095.33
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
제품 설명
In Vitro
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. Further protocols information, click here.
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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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분자량 1095.33
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
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)
Protocol
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Phalloidin F-actin cytoskeleton staining
Phalloidin F-actin staining detects polymerized filamentous actin in fixed and permeabilized specimens by using fluorescent phalloidin or phalloidin-derived phallotoxins that bind actin filaments and generate a fluorescence microscopy readout corresponding to F-actin organization, including stress fibers, cortical actin, filament bundles, and tissue-specific actin networks. Phalloidin stabilizes F-actin by reducing actin subunit dissociation from filament ends, and fluorescent phallotoxins were established as tools for visualizing actin-containing structures in eukaryotic cells.
순도&문서
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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 |
AA-BR-157 Related Classifications
HY-168969 Related Classifications
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