PROTAC BRD4 Degrader-44
PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC50 of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Formula: C39H38ClN7O8S
- Molecular Weight:800.28
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
|
BRD4 |
PROTAC BRD4 Degrader-44 (Compound 2a) (1 μM; 0.5-6 h) exhibits high stability in medium containing 10% FBS and moderate stability in mouse liver microsomes without NADPH; only 1.70% of the compound remains after incubation for 30 min in the presence of NADPH[1].
PROTAC BRD4 Degrader-44 (10 μM; 0.5-6 h) accumulates in MCF-7 cells, with intracellular concentrations higher than those of dBET1 at all tested time points, and reaches levels comparable to its diastereomer after 6 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 cells
-
Concentration:10, 30, 100, 300, 1000, 3000, 10000 nM
-
Incubation Time:4 h
-
Result:Exhibited a half-maximal degradation concentration (DC50) of 16 nM, representing approximately a 5-fold enhancement in BRD4 degradation activity compared to dBET1.
Showed a hook effect.
Chemical Information
-
Molecular Weight 800.28
-
Formula C39H38ClN7O8S
-
SMILES
CC1=C(SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N24)C)CC(O[C@@H](CCC(NCCOC5=CC=CC(C6=O)=C5C(N6C7C(NC(CC7)=O)=O)=O)=O)C)=O)C
-
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)