LAG-3 PROTAC-1
LAG-3 PROTAC-1 is a lymphocyte activation gene-3 (LAG-3) PROTAC degrader with a DC50 of 0.27 μM. LAG-3 PROTAC-1 induces the formation of a ternary complex with LAG-3 and CRL4CRBN, promoting proteasomal degradation. LAG-3 PROTAC-1 is applicable for cancer-related research.
(Pink: LAG-3 ligand (HY-179061); Blue: Cereblon ligand (HY-10984); Black: linker).
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- Formule: C34H36N6O5
- Masse moléculaire:608.69
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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
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Activité biologique
Description
IC50 & Target
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Cereblon |
In Vitro
LAG-3 PROTAC-1 (0.001-10 μM; 24 h) potently and selectively induces dose-dependent degradation of LAG-3 in Raji-LAG3 cells with a DC50 of 0.27 μM[1].
LAG-3 PROTAC-1 forms a stable, conformationally favorable complex with purified LAG-3, as demonstrated by 100 ns MD simulations, with key binding interactions that support ternary complex formation with CRL4CRBN[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Raji-LAG3 cells (LAG-3-expressing Raji cells)
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Induced potent, dose-dependent degradation of LAG-3 protein levels, with a maximum reduction of up to 85% at 10 μM.
Confirmed degradation to be CRL4CRBN-dependent, as co-treatment with the NAE inhibitor MLN4924 rescued LAG-3 levels.
Showed no degradation in Raji-Null cells lacking LAG-3, confirming target specificity.
Achieved a DC50 of 0.27 μM.
Chemical Information
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Masse moléculaire 608.69
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Formule C34H36N6O5
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SMILES
O=C(NCCCCNC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)[C@H]([C@@H](C4=CC=CC=C4)C5)CN5CC6=CC=CC=N6
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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)
LAG-3 PROTAC-1 Related Classifications
HY-179060 Related Classifications
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