Breceptin
Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer.
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。
- CAS 番号: 215713-39-6
- 分子式: C136H200N38O28
- 分子量:2815.28
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Bradykinin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
Bradykinin B1 Receptor (B1R) |
Bradykinin B2 Receptor (B2R) |
ERK1 |
ERK2 |
化学情報
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CAS 番号 215713-39-6
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分子量 2815.28
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分子式 C136H200N38O28
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SMILES
O=C(NCC(N[C@H](C(N[C@H](C(N[C@@H](C(N1[C@@]2([C@]([H])(C[C@H]1C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)CCCC2)[H])=O)C3CC4=C(C3)C=CC=C4)=O)CO)=O)C5CC6=C(C5)C=CC=C6)=O)[C@H]7N(C([C@H]8N(C([C@@H](NC([C@H](NC(CCCCCCC(N[C@@H](C(N[C@H](C(N9[C@H](C(N%10[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@@H](C(N%11[C@@]%12([C@]([H])(C[C@H]%11C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)CCCC%12)[H])=O)C%13CC%14=C(C%13)C=CC=C%14)=O)CO)=O)C%15CC%16=C(C%15)C=CC=C%16)=O)=O)C[C@H](C%10)O)=O)CCC9)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCC8)=O)C[C@@H](C7)O
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別名
B 9870
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)