CG 858-Neg
CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAFV600E with Ki values of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAFV600E-driven melanoma (e.g., A375 cells, IC50=492 nM) and colorectal cancer (e.g., HT-29 cells, IC50=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2417296-83-2
- Formula: C43H41F2N7O8S
- Molecular Weight:853.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
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Cereblon |
B-RafV600E |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
492 nM
Compound: 13
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Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
In Vitro
CG 858-Neg (compound 13) is unable to bind to cereblon due to partial N-methylation of the thalidomide moiety[1].
CG 858-Neg (1-1000 nM; 16 h) does not degrade BRAFV600E and partially suppresses downstream ERK phosphorylation; at 37-1000 nM, it can inhibit the phosphorylation of downstream p-ERK in A375 cells[1].
CG 858-Neg (1000 nM; 7 days) inhibits colony formation of A375 cells at concentrations of 200 nM and above[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:A375 melanoma cells
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Concentration:1-1000 nM
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Incubation Time:16 h
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Result:Did not induce degradation of BRAF-V600E protein levels at any tested concentration; suppressed p-ERK levels in a dose-dependent manner.
Chemical Information
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CAS No. 2417296-83-2
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Molecular Weight 853.89
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Formula C43H41F2N7O8S
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SMILES
O=C(C1=C(F)C(NS(=O)(CCC)=O)=CC=C1F)C2=CNC3=NC=C(C4=CC=C(CNC(CCCCNC5=CC=C6C(N(C7C(N(C)C(CC7)=O)=O)C(C6=C5)=O)=O)=O)C=C4)C=C32
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)