2. PROTAC
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  4. AA-BR-157

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)).

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AA-BR-157

AA-BR-157 構造式

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 3108 在庫あり
Solution
10 mM * 1 mL in DMSO USD 3108 在庫あり
Solid
1 mg $640 在庫あり
5 mg $1610 在庫あり
10 mg $2580 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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AA-BR-157 関連抗体

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PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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製品説明

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[1]. (Pink: MT2A ligand (HY-168970); Blue: VHL ligand (HY-125845); Black: linker (HY-119429)).

体外実験

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.

AA-BR-157 関連抗体

Western Blot Analysis[1]

Cell Line: stable MT2A-V5 overexpressing MDA-MB-231 (MT2A OE) cells
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30 μM (24 h incubation); 10 μM (time-course analysis)
Incubation Time: 24 h (dose-dependent assay); varying times (time-course analysis)
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.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells, U-87 MG cells
Concentration: 0, 1, 3, 10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 3, 10 μM
Incubation Time: 24 h
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.
分子量

1095.33

分子式

C56H70N8O11S2
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
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
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9130 mL 4.5648 mL 9.1297 mL
5 mM 0.1826 mL 0.9130 mL 1.8259 mL
10 mM 0.0913 mL 0.4565 mL 0.9130 mL
View the 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.

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純度とドキュメンテーション
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
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AA-BR-157 Related Classifications

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AA-BR-157PROTACsproteasomal degradationcytoskeletal remodelingMetallothionein 2AMT2AU-87 MG cellsglioblastomatriple negative breast cancerC44MDA-MB-231 cellsDIAPH3Inhibitorinhibitorinhibit

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製品名:
AA-BR-157
製品番号:
HY-168969
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