[CAS NO. 2413382-30-4] BRD4 degrader-3
PRODUCTS SPECIFICATIONS [2413382-30-4]
DESCRIPTION [2413382-30-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 475.61 |
| Molecular Formula | C26H29N5O2S |
| SMILES | O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(C#CCN)C=C4)=N1 |
Summary
PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC 50 s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively [1] . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IC50 & Target
|
BRD4 BD1 15.5 nM (IC 50 ) |
BRD4 BD2 12.3 nM (IC 50 ) |
In Vitro
PROTAC BRD4 Degrader-7 shows an IC 50 of 27.1 nM in BRD4 Full Length Binding assay. PROTAC BRD4 Degrader-7 degrades BRD4 with an EC 50 of 1.4 nM for PC3-Steapl cells and an IC 50 of 1.3 nM for EoL-1 Cells. PROTAC BRD4 Degrader-7 inhibits PC-3-STEAP-1 and EoL-l proliferation with IC 50 s of 6.6 and 2.2 nM, respectively. PROTAC BRD4 Degrader-7 inhibits MYC expression in MV-4-11 cells with an IC 50 of 2.9 nM [1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.