PROTAC BRD4-binding moiety 1

• CAT Number: I015438
• CAS Number: 2101200-10-4
• Molecular Formula: C23H21N3O2
• Molecular Weight: 371.43
• Purity: ≥95%
• Synonyms: 6-(3,5-dimethyl-1,2-oxazol-4-yl)-1-methyl-4-phenyl-3-prop-2-ynyl-4H-quinazolin-2-one
• InChI: InChI=1S/C23H21N3O2/c1-5-13-26-22(17-9-7-6-8-10-17)19-14-18(21-15(2)24-28-16(21)3)11-12-20(19)25(4)23(26)27/h1,6-12,14,22H,13H2,2-4H3
• InChIKey: ZKJVDZJHVLJOKO-UHFFFAOYSA-N
• SMILES: CC1=C(C(=NO1)C)C2=CC3=C(C=C2)N(C(=O)N(C3C4=CC=CC=C4)CC#C)C

PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136)[1]. PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1[1].

Reference

[1]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228.
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