PROTAC BRD2/BRD4 degrader-1
Product Specifications
UNSPSC Description
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A[1].
Target Antigen
Epigenetic Reader Domain; PROTACs
Type
Reference compound
Related Pathways
Epigenetics;PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-brd2-brd4-degrader-1.html
Solubility
10 mM in DMSO
Smiles
O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC4=CC5=C(NS(=O)(C6=CC=CC=C6OC)=O)C=CC(N(C)C7=O)=C5C7=C4
Molecular Weight
766.82
References & Citations
[1]Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181.
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-130612/PROTAC-BRD2-BRD4-degrader-1-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-130612/
Clinical Information
No Development Reported
CAS Number
2570470-42-5
Curated Selection
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