PROTAC BRD4-binding moiety 1

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).

Product information

CAS Number: 2101200-10-4

Molecular Weight: 371.43

Formula: C23H21N3O2

Chemical Name: 6-(3, 5-dimethyl-1, 2-oxazol-4-yl)-1-methyl-4-phenyl-3-(prop-2-yn-1-yl)-1, 2, 3, 4-tetrahydroquinazolin-2-one

Smiles: CN1C(=O)N(CC#C)C(C2=CC(=CC=C12)C1=C(C)ON=C1C)C1=CC=CC=C1

InChiKey: ZKJVDZJHVLJOKO-UHFFFAOYSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1.

References:

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.

Products are for research use only. Not for human use.