PROTAC BRD4 Degrader-51
PROTAC BRD4 Degrader-51 is a PROTAC-class degrader targeting BRD4, which degrades BRD4 via the ubiquitin-proteasome pathway. PROTAC BRD4 Degrader-51 degrades BRD4 (long) and BRD4 (short) isoforms with DC50 values of 27.92 nM and 20.03 nM, respectively. PROTAC BRD4 Degrader-51 exhibits antiproliferative activity against tumor cells. It can be used in research related to various cancers such as leukemia and breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-W674436); Black: linker).
For research use only. We do not sell to patients.
- Formula: C44H50ClN9O7S
- Molecular Weight:884.44
-
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
|
BRD4 |
PROTAC BRD4 Degrader-51 (compound 1) (72 h) potently inhibits the proliferation of MV411, K562, MDA-MB-231, MDA-MB-453, SK-BR-3, AGS and MIA PaCa-2 tumor cells, with IC50 values ranging from 0.10 μM to 4.71 μM[1].
PROTAC BRD4 Degrader-51 (6.25-100 nM; 16 h) potently degrades BRD4 (long) and BRD4 (short) isoforms in MV411 cells, with DC50 values of 27.92 nM and 20.03 nM, respectively[1].
PROTAC BRD4 Degrader-51 (50 nM; 16 h) mediates BRD4 degradation in MV411 cells via the proteasome pathway, with degradation dependent on the recruitment of E3 ligase; it induces ubiquitination of BRD4 in MV411 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MV411
-
Concentration:6.25, 12.5, 25, 50, 100 nM
50 nM (8 h time point) -
Incubation Time:16 h
8 h (50 nM concentration) -
Result:Induced dose-dependent degradation of both BRD4(long) and BRD4 (short) isoforms.
Achieved a DC50 of 27.92 nM for BRD4 (long) with a maximum degradation (DMAX) of 89.46%, and a DC50 of 20.03 nM for BRD4 (short) with a DMAX of 78.38%.
Observed degradation starting at 8 h with 50 nM of the compound.
-
Cell Line:MV411
-
Concentration:50 nM
2 μM (MG132 (HY-13259) pre-treatment) -
Incubation Time:16 h
2 h (MG132) -
Result:Inhibited the degradation of both BRD4 (long) and BRD4 (short) isoforms induced by PROTAC BRD4 Degrader-51 when cells were pre-treated with proteasome inhibitor, restoring BRD4 protein levels to near control levels.
-
Cell Line:MV411
-
Concentration:50 nM
250 nM (Lenalidomide (HY-A0003)) -
Incubation Time:16 h
-
Result:Inhibited the degradation of both BRD4 (long) and BRD4 (short) isoforms induced by PROTAC BRD4 Degrader-51 when cells were co-treated with lenalidomide, restoring BRD4 protein levels to near control levels.
-
Cell Line:MV411
-
Concentration:50 nM
-
Incubation Time:16 h
-
Result:Increased the level of ubiquitinated BRD4 compared to untreated control cells.
Chemical Information
-
Molecular Weight 884.44
-
Formula C44H50ClN9O7S
-
SMILES
CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCCN(C)CCCCNC(CCCCOC5=C(C(N([C@@H]6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)=O
-
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-51 Related Classifications
HY-187372 Related Classifications
Powered by Bioz