CRBN ligand-908
CRBN ligand-908 is a cereblon (CRBN) ligand and also a HaloTag-binding degrader. CRBN ligand-908 competes with fluorescent lenalidomide ligands for binding to full-length CRBN protein. CRBN ligand-908 contains a chlorohexyl group that covalently reacts with HaloTag fused to target proteins. CRBN ligand-908 induces degradation of HaloTag-fused FAK, endogenous MARC1, and BRD4 proteins. CRBN ligand-908 is a proteasome- and Cullin-dependent degrader. CRBN ligand-908 does not induce degradation of the novel CRBN substrates GSPT1, SALL4, or CSNK1α. CRBN ligand-908 can be used to synthesize PROTACs, such as HaloPROTAC 4 (HY-187337).
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- Formel: C32H39N5O3
- Molecular Weight:541.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Cereblon |
CRBN ligand-908 (compound 14) (24 h) potently degrades FAK-HaloTag-HiBiT in A549 cells with a pDC50 of 7.91 and 58.8% maximum degradation after 24 h[1].
CRBN ligand-908 (6 h) does not degrade the CRBN neosubstrates GSPT1, SALL4, or CSNK1α in HEK293 or SK-N-DZ cells after 6 h treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 541.68
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Formel C32H39N5O3
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SMILES
O=C1NC(CCN1C2=CC=CC3=C2C=CN3C4CCN(CCC5CCN(C(C6=CC=C(C)C=C6)=O)CC5)CC4)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)