Umckalin
Umckalin is Coumarin (HY-N0709) derivative that exhibits anti-inflammatory properties. Umckalin reduces phosphorylation of p38 MAPK, JNK, and ERK, lowers TNF-α, IL-6, IL-1β, NO, and PGE2 production. Umckalin can be used for the research of chronic inflammatory diseases.
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- CAS No.: 43053-62-9
- Formule: C11H10O5
- Masse moléculaire:222.19
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
Umckalin (25-400 µM; 72 h) does not reduce viability of B16F10 murine melanoma cells at concentrations up to 200 µM[2].
Umckalin (50-200 µM; 72 h) dose-dependently increases intracellular melanin content in B16F10 murine melanoma cells[2].
Umckalin (50-200 µM; 72 h) dose-dependently enhances tyrosinase activity in B16F10 murine melanoma cells[2].
Umckalin (50-200 µM; 24 h) upregulates TRP-1 and MITF protein expression in B16F10 murine melanoma cells, while having minimal to no effect on tyrosinase and TRP-2 expression[2].
Umckalin (50-200 µM; 24 h) activates the GSK-3β/β-catenin pathway in B16F10 murine melanoma cells by increasing Ser9 phosphorylation of GSK-3β, reducing β-catenin phosphorylation, and increasing total β-catenin levels[2].
Umckalin (50-200 µM; 4 h) suppresses MAPK pathway activity in B16F10 murine melanoma cells by reducing ERK and JNK phosphorylation, while not affecting p38 phosphorylation[2].
Umckalin (50-200 µM; 4 h) activates the PI3K/AKT pathway in B16F10 murine melanoma cells by increasing PI3K and AKT phosphorylationn[2].
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:B16F10 murine melanoma cells
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Concentration:25; 50; 100; 200; 400 µM
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Incubation Time:72 h
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Result:Showed no cytotoxic effects at concentrations up to 200 µM.
Caused significant cytotoxicity at 400 µM.
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Cell Line:B16F10 murine melanoma cells
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Concentration:50; 100; 200 µM
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Incubation Time:24 h
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Result:Increased TRP-1 protein expression significantly in a dose-dependent manner (p < 0.001 at all concentrations).
Caused a small but significant increase in tyrosinase expression only at 200 µM.
Had no notable effect on TRP-2 expression.
Increased MITF protein expression significantly in a dose-dependent manner.
Increased Ser9 phosphorylation of GSK-3β significantly in a dose-dependent manner.
Increased total β-catenin levels significantly only at 200 µM.
Reduced β-catenin phosphorylation significantly at 200 µM.
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Cell Line:B16F10 murine melanoma cells
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Concentration:50-200 µM
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Incubation Time:4 h
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Result:Reduced ERK phosphorylation significantly in a dose-dependent manner.
Reduced JNK phosphorylation significantly in a dose-dependent manner.
Had no significant effect on p38 phosphorylation.\nIncreased PI3K phosphorylation significantly in a dose-dependent manner.
Increased AKT phosphorylation significantly in a dose-dependent manner.
Chemical Information
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CAS No. 43053-62-9
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Masse moléculaire 222.19
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Formule C11H10O5
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SMILES
O=C1C=CC2=C(OC)C(OC)=C(O)C=C2O1
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Structure Classification
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Initial Source
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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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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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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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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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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Umckalin Related Classifications
HY-N8712 Related Classifications
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