PROTAC BRD4 Degrader-1 is an efficacious BRD4 degrader with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.

Product information

CAS Number: 2133360-00-4

Molecular Weight: 771.78

Formula: C40H37N9O8

Chemical Name: 2-[2-(4-{[6-(3,5-dimethyl-1,2-oxazol-4-yl)-1-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydroquinazolin-3-yl]methyl}-1H-1,2,3-triazol-1-yl)ethoxy]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide

Smiles: CN1C2=CC=C(C=C2C(C2C=CC=CC=2)N(CC2=CN(CCOCC(=O)NC3=CC=CC4=C3C(=O)N(C3CCC(=O)NC3=O)C4=O)N=N2)C1=O)C1C(C)=NOC=1C

InChiKey: FXNACIMQXOPNJG-UHFFFAOYSA-N

InChi: InChI=1S/C40H37N9O8/c1-22-34(23(2)57-44-22)25-12-13-30-28(18-25)36(24-8-5-4-6-9-24)48(40(55)46(30)3)20-26-19-47(45-43-26)16-17-56-21-33(51)41-29-11-7-10-27-35(29)39(54)49(38(27)53)31-14-15-32(50)42-37(31)52/h4-13,18-19,31,36H,14-17,20-21H2,1-3H3,(H,41,51)(H,42,50,52)

Technical Data

Appearance: Solid Power

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

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: ≥12 months 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-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC50 value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines. PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration.

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