C9S
C9S is an As (III)-PROTAC and arsenic-binding protein PROTAC degrader. C9S promotes the ubiquitination and degradation of arsenic-binding proteins such as Glutathione reductase. C9S binds to metallothionein. C9S exhibits anticancer activity against lung cancer. C9S can be used in lung cancer-related research.
(Pink: Glutathione Reductase (GR) Target protein ligand; Blue: Cereblon ligand (HY-103597); Black: linker (HY-B0236)).
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- Formule: C29H31AsN4O7S2
- Masse moléculaire:686.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Cereblon |
C9S (2 μM; 1 h) directly binds to purified metallothionein in in vitro protein-binding assays[1].
C9S (10-40 μM; 24 h) is taken up by lung cancer cell line A549 in a concentration-dependent manner, and its uptake efficiency at concentrations of 10, 20 and 40 μM is significantly higher than that of the C9 probe after 24 h of incubation[1].
C9S (5-80 μM; 24 h) does not significantly reduce the viability of lung cancer A549 cells at concentrations up to 40 μM after 24 h of incubation, but induces significant cytotoxicity at concentrations of 60 μM and 80 μM[1].
Treatment of lung cancer A549 cells with C9S (40 μM; 24 h) downregulates 135 proteins, most of which contain potential arsenic-binding cysteine residues, and these proteins are enriched in key cellular metabolism and DNA processing pathways[1].
Treatment of lung cancer cell line A549 with C9S (40 μM; 24 h) induces GSR degradation mediated by the ubiquitin-proteasome system and significantly downregulates the protein levels of EED and PLAA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human lung carcinoma cells
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Concentration:5, 10, 20, 40, 60, 80 μmol/L
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Incubation Time:24 h
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Result:Did not cause significant cytotoxicity at concentrations from 0 to 40 μmol/L.
Decreased cell viability to 70% at 60 μmol/L, with the reduction statistically significant compared to controls.
Decreased cell viability to 57% at 80 μmol/L, with the reduction statistically significant compared to controls.
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Cell Line:A549 human lung carcinoma cells
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Concentration:40 μmol/L (C9S); 10 μmol/L (MG132 pretreatment)
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Incubation Time:24 h (C9S incubation); 2 h (MG132 pretreatment)
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Result:Significantly downregulated expression of glutathione reductase (GSR), embryonic ectoderm development (EED), and phospholipase A-2-activating protein (PLAA).
Diminished downregulation of GSR with pretreatment of proteasome inhibitor MG132, confirming ubiquitin-proteasome system-mediated degradation.
Reduced EED expression, with the reduction statistically significant.
Reduced PLAA expression, with the reduction statistically significant.
Chemical Information
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Masse moléculaire 686.63
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Formule C29H31AsN4O7S2
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SMILES
O=C(CC1)NC(C1N(C2=O)C(C(C2=CC=C3)=C3OCC(NCCCCCC(NC4=CC=C([As]5SCCS5)C=C4)=O)=O)=O)=O
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)