PROTAC BRD4 Degrader-29
PROTAC BRD4 Degrader-29 is a potent BRD4 PROTAC degrader with a DC50 of 89.4 nM. PROTAC BRD4 Degrader-29 mediates proteasomal degradation of BRD4 by bridging BRD4 and the CRBN E3 ubiquitin ligase. PROTAC BRD4 Degrader-29 can be used in cancer research.
(Pink: BRD4 ligand (HY-13030); Blue: Cereblon ligand (HY-103597); Black: linker (HY-172125)).
For research use only. We do not sell to patients.
- Formula: C58H61ClN10O9S2
- Molecular Weight:1141.75
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
BRD4 89.4 nM (DC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | DC50 |
89.4 nM
|
BRD4 degradation in HEK293 CRISPR HiBiT BRD4 cells assessed by Nano-Glo HiBiT assay after 18 h of incubation.
BRD4 degradation in HEK293 CRISPR HiBiT BRD4 cells assessed by Nano-Glo HiBiT assay after 18 h of incubation.
|
39967623 |
In Vitro
PROTAC BRD4 Degrader-29 (Compound 7a) (0.001-10 μM; 18 h) efficiently degrades BRD4 in HEK293 CRISPR HiBiT BRD4 cells with a DC50 of 89.4 nM. It also degrades the BRD4 long and BRD4 short isoforms in parental HEK293 cells, and its degradation activity can be reversed by the proteasome inhibitor MG132 (HY-13259), neddylation inhibitor MLN4924 (HY-70062), and CRBN ligand competitor Thalidomide (HY-14658)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293 parental cell line
-
Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
-
Incubation Time:18 h
-
Result:Visibly degraded both BRD4 long and BRD4 short isoforms in the range of 0.3-1 μM, and this degradation was reversed by the addition of MG132, MLN4924, or thalidomide, confirming its dependence on the proteasome and CRBN ubiquitin ligase pathways.
Chemical Information
-
Molecular Weight 1141.75
-
Formula C58H61ClN10O9S2
-
SMILES
CC1=NN=C2N1C3=C(C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCCNC(C5=CC=C(SCCC#CC(C6CCOCC6)N7CCC(NC(COC8=CC=CC9=C8C(N(C%10CCC(NC%10=O)=O)C9=O)=O)=O)CC7)C=C5)=O)=O)C(C)=C(C)S3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC BRD4 Degrader-29 Related Classifications
HY-172124 Related Classifications
Powered by Bioz