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.
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- CAS No.: 215713-39-6
- Formule: C136H200N38O28
- Masse moléculaire:2815.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
Bradykinin B1 Receptor (B1R) |
Bradykinin B2 Receptor (B2R) |
ERK1 |
ERK2 |
Chemical Information
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CAS No. 215713-39-6
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Masse moléculaire 2815.28
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Formule 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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Synonyms
B 9870
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)