2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs Glutathione Reductase (GR)
  4. 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)).

For research use only. We do not sell to patients.

C9S

C9S Chemical Structure

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C9S Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: Glutathione Reductase (GR) Target protein ligand; Blue: Cereblon ligand (HY-103597); Black: linker (HY-B0236)).

IC50 & Target[1]

Cereblon

 

In Vitro

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.

C9S Related Antibodies

Cell Viability Assay[1]

Cell Line: A549 human lung carcinoma cells
Concentration: 5, 10, 20, 40, 60, 80 μmol/L
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: A549 human lung carcinoma cells
Concentration: 40 μmol/L (C9S); 10 μmol/L (MG132 pretreatment)
Incubation Time: 24 h (C9S incubation); 2 h (MG132 pretreatment)
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.
Molecular Weight

686.63

Formula

C29H31AsN4O7S2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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C9S Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

C9SPROTACsGlutathione Reductase (GR)Glutathione Reductasephospholipase A-2-activating proteinglutathione reductaselung carcinoma cellsA549 human lung carcinoma cellsmetallothioneinembryonic ectoderm development proteinubiquitin-proteasome systemcysteine residuesInhibitorinhibitorinhibit

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