GSPT1 degrader-11
GSPT1 degrader-11 is a CRBN-dependent molecular glue degrader targeting GSPT1, with a DC50 of 67.7 nM. GSPT1 degrader-11 induces CRBN-dependent degradation of GSPT1 via the ubiquitin-proteasome pathway. GSPT1 degrader-11 exhibits CRBN-dependent growth inhibitory activity in cancer cells. GSPT1 degrader-11 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C41H45N11O5
- Molecular Weight:771.87
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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All Eukaryotic Release Factor (eRF) Isoforms
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Biological Activity
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eRF3a/GSPT1 67.7 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | IC50 |
1.1 μM
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Growth inhibitory activity against human MDA-MB-231 CRBN-WT cells assessed after 72 h incubation via cell viability assay.
Growth inhibitory activity against human MDA-MB-231 CRBN-WT cells assessed after 72 h incubation via cell viability assay.
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40432221 |
| MDA-MB-231 | IC50 |
2.07 μM
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Growth inhibitory activity against human MDA-MB-231 CRBN-WT cells assessed via cell viability assay in a head-to-head comparison.
Growth inhibitory activity against human MDA-MB-231 CRBN-WT cells assessed via cell viability assay in a head-to-head comparison.
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40432221 |
| MDA-MB-231 | DC50 |
67.7 nM
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GSPT1 degradation activity in human MDA-MB-231 CRBN-WT cells assessed after 24 h treatment via Western blot analysis, with 97% maximum degradation efficacy.
GSPT1 degradation activity in human MDA-MB-231 CRBN-WT cells assessed after 24 h treatment via Western blot analysis, with 97% maximum degradation efficacy.
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40432221 |
GSPT1 degrader-11 (Comp 12-60) (at -log 0.5-log 1.5 μM for 72 h) potently and selectively inhibits the proliferation of MDA-MB-231 CRBN-WT cells in a CRBN-dependent manner, with an IC50 value of 1.1 μM[1].
GSPT1 degrader-11 (0-10 μM; 12-24 h) induces dose-dependent and CRBN-dependent degradation of GSPT1 in MDA-MB-231 cells via the ubiquitin-proteasome pathway, with a DC50 of 67.7 nM and a maximum degradation efficiency of 97%[1].
GSPT1 degrader-11 binds directly to recombinant GSPT1 protein, with a KD value of 2.4 μM[1].
GSPT1 degrader-11 (1 μM; 72 h) alters the expression of genes involved in translation regulation, ribosome biogenesis and other cellular processes in MDA-MB-231 cells, which is consistent with the biological function of its target GSPT1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 CRBN wild-type (CRBN-WT) and CRBN knockout (CRBN-KO) cells
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Concentration:-log 0.5, log 0, log 0.5, log 1, log 1.5 μM
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Incubation Time:72 h
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Result:Potently inhibited MDA-MB-231 CRBN-WT cell growth with an IC50 of 1.1 μM.
Showed no effect in CRBN-KO cells.
Exhibited a comparable growth inhibitory IC50 of 2.07 μM in a head-to-head comparison with CC-90009 (HY-130800).
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Cell Line:MDA-MB-231 CRBN wild-type (CRBN-WT) and CRBN knockout (CRBN-KO) cells
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Concentration:0, 0.1, 0.3, 1, 3, 10 μM
1 μM (with 10 μM proteasome inhibitor or 0.3 μM NEDD8-activating enzyme inhibitor cotreatment) -
Incubation Time:24 h
12 h (cotreatment) -
Result:Induced dose-dependent degradation of GSPT1 in MDA-MB-231 CRBN-WT cells.
Showed no GSPT1 degradation in CRBN-KO cells.
Blocked GSPT1 degradation by cotreatment with proteasome inhibitor or NEDD8-activating enzyme inhibitor.
Induced near-complete GSPT1 degradation with a Dmax of 97% and a DC50 of 67.7 nM in a head-to-head comparison with cereblon E3 ligase modulator CC-90009.
Chemical Information
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Molecular Weight 771.87
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Formula C41H45N11O5
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(N4CC(N5CCC(C(N6CCN(C7=CC=C(NC8=NC=C9N=C(C%10CC%10)N(C)C9=N8)C=C7)CC6)=O)CC5)C4)=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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSPT1 degrader-11 Related Classifications
HY-177724 Related Classifications
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