GSPT1 degrader-13
GSPT1 degrader-13 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-13 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-13 can be used for leukemia research.
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- Formule: C22H23ClN4O6S
- Masse moléculaire:506.96
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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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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform Eukaryotic Release Factor (eRF)
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Activité biologique
Description
IC50 & Target
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eRF3a/GSPT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BE(2)-C | EC50 |
12 μM
Compound: 1
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Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
| MOLT-4 | EC50 |
0.18 μM
Compound: 1
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Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
| MV4-11 | EC50 |
0.19 μM
Compound: 1
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Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
In Vitro
GSPT1 degrader-13 (compound 1) (3 days) exhibits anti-proliferative activity against cancer cells, with EC50s of 0.18 (MOLT4), 0.19 (MV4;11), and 12 μM (BE(2)-C)[1].
GSPT1 degrader-13 (3 h) shows GSPT1 degradation activity in MOLT4, MV4;11, and BE(2)-C cells, with EC50s of 0.28, 0.28, and 8 μM, respectively[1].
GSPT1 degrader-13 (3 μM, 3 h) degrades GSPT1 in wild-type MOLT4, MV4;11, and BE(2)-C cells, but its degradation activity is blocked by CRBN KO cells and G575N mutant cells, indicating that it degrades GSPT1 in a CRBN- and GSPT1-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 506.96
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Formule C22H23ClN4O6S
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SMILES
O=C(N1)C(N2CC3=CC(NS(=O)(NCCOC4=C(C=CC=C4C)Cl)=O)=CC=C3C2=O)CCC1=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)
GSPT1 degrader-13 Related Classifications
HY-177752 Related Classifications
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