A cereblon modulator with an IC50 value of 60 nM in a competitive TR-FRET assay; has a higher affinity for cereblon than the related modulators lenalidomide (IC50 = 1

Iberdomide – 5 mg

Brand:
Cayman
CAS:
1323403-33-3
Storage:
-20
UN-No:
Non-Hazardous - /

Iberdomide is a modulator of cereblon, a substrate receptor in the CRL4 ubiquitin ligase complex, that has an IC50 value of 60 nM in a competitive TR-FRET assay.{39212} In the same assay, it has a higher affinity for cereblon than the related modulators lenalidomide (Item No. 14643; IC50 = 1,500 nM) and pomalidomide (Item No. 19877; IC50 = 1,200 nM). Iberdomide also has a greater potency for degrading the CRL4 complex substrates Ikaros and Aiolos (EC50s = 1 and 0.5 nM) but has no degradative activity for GSPT1 or CK1α.  

 

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Description

A cereblon modulator with an IC50 value of 60 nM in a competitive TR-FRET assay; has a higher affinity for cereblon than the related modulators lenalidomide (IC50 = 1,500 nM) and pomalidomide (IC50 = 1,200 nM) in the same assay; has a greater potency for degradation of the CRL4 complex substrates Ikaros and Aiolos (EC50s = 1 and 0.5 nM) as well; does not degrade GSPT1 or CK1α ,

Formal name: 3S-[1,3-dihydro-4-[[4-(4-morpholinylmethyl)phenyl]methoxy]-1-oxo-2H-isoindol-2-yl]-2,6-piperidinedione

Synonyms:  CC-220

Molecular weight: 449.5

CAS: 1323403-33-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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