MG degrader 3
MG degrader 3 is a molecular glue degrader that induces the degradation of multiple proteins including GSPT1, ZFP91 and CK1α via the ubiquitin-proteasome system, regulates protein stability and cellular signaling networks, and exhibits anti-proliferative activity against multiple myeloma cells. MG degrader 3 can be applied in the research of multiple myeloma.
For research use only. We do not sell to patients.
- CAS No.: 2413733-73-8
- Formula: C24H24ClN3O5
- Molecular Weight:469.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GSPT1 |
ZFP91 |
CK1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
8.7 nM
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Antiproliferative activity against multiple myeloma MM.1S cells assessed as inhibition of cell viability.
Antiproliferative activity against multiple myeloma MM.1S cells assessed as inhibition of cell viability.
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40131988 |
In Vitro
MG degrader 3 (CM-3) potently inhibits MM.1S cell viability with an IC50 of 8.7 nM[1].
MG degrader 3 (CM-3) (1 μM; 4-16 h) induces time-dependent degradation of ZFP91 in MM.1S cells, with observable reduction starting at 4 h post-treatment[1].
MG degrader 3 (CM-3) binds to the tritryptophan pocket of CRBN with an IC50 of 382.24 nM, exhibiting higher affinity than lenalidomide[1].
MG degrader 3 (CM-3) induces the formation of neo-protein-protein interactions between CRBN and multiple proteins including GSPT1, CSNK1A1, ZFP91, PI4KB, PPIL4, MNAT1, and FAM83G in HEK293T cells[1].
MG degrader 3 (CM-3) (1 μM; 1-24 h) induces CRL4CRBN-dependent, proteasome-mediated degradation of ZFP91, CSNK1A1, and GSPT1 in HEK293T cells, with an observable effect on ZFP91 starting at 4 h post-treatment[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:HEK293T cells
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Concentration:1 μM (time-dependent degradation assays; mechanism validation)
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Incubation Time:1, 4, 8, 12, 24 h (time-dependent degradation assays); 8 h (mechanism validation)
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Result:Induced time-dependent degradation of ZFP91 (obvious reduction after 4 h treatment), CSNK1A1 (marked reduction after 24 h treatment), and GSPT1 (marked reduction after 24 h treatment).
Degradation of ZFP91 was blocked by pretreatment with ubiquitin activating enzyme E1 inhibitor MLN7243, NEDD8 activating enzyme inhibitor MLN4924, or proteasome inhibitor MG132.
Caused slight downregulation of PI4KB after 24 h treatment.
Showed no observable degradation of MNAT1 and PPIL4.
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Cell Line:multiple myeloma MM.1S cells
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Concentration:1 μM
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Incubation Time:4, 8, 16 h
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Result:Induced time-dependent degradation of ZFP91, with reduced abundance observed starting at 4 h post-treatment.
Chemical Information
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CAS No. 2413733-73-8
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Molecular Weight 469.92
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Formula C24H24ClN3O5
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SMILES
O=C(NC1=CC=C(C)C(Cl)=C1)CCCOC2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O
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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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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MG degrader 3 Related Classifications
HY-177728 Related Classifications
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Keywords
- MG degrader 3
- 2413733-73-8
- MG degrader3
- MG degrader-3
- Molecular Glues
- Creatine Kinase
- PI4KB
- ubiquitin-proteasome system pathway
- casein kinase I alpha (CSNK1A1/CK1α)
- MM.1S cell
- HEK293T cells
- multiple myeloma cells
- CRL4CRBN
- cereblon (CRBN)
- eukaryotic peptide chain release factor (GSPT1)
- zinc finger protein 91 (ZFP91)
- Inhibitor
- inhibitor
- inhibit