PROTAC BRD4 Degrader-38
PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50 values of 86 nM and 106 nM against the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 covalently binds to the Cys232 residue of TRIM28 to form a ternary complex containing BRD4, thereby promoting the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-38 can be used in the research of acute myeloid leukemia.
(Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-203082); Black: linker (HY-40172)).
For research use only. We do not sell to patients.
- Formula: C31H30ClN7O4S
- Molecular Weight:632.13
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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]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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BRD4 86 nM (DC50, BRD4-S) |
BRD4 106 nM (DC50, BRD4-L) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
86 nM
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Degradation of BRD4 short isoform in human HEK293T cells after 16 h of treatment.
Degradation of BRD4 short isoform in human HEK293T cells after 16 h of treatment.
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40464197 |
| HEK-293T | DC50 |
106 nM
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Degradation of BRD4 long isoform in human HEK293T cells after 16 h of treatment.
Degradation of BRD4 long isoform in human HEK293T cells after 16 h of treatment.
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40464197 |
PROTAC BRD4 Degrader-38 (Compound 4090) (10 nM) potently degrades BRD4 protein in K562, Daudi and MV-4-11 cancer cell lines[1].
PROTAC BRD4 Degrader-38 (0.1-2 μM; 16 h) potently induces proteasome-dependent degradation of the short isoform (DC50 = 86 nM) and long isoform (DC50 = 106 nM) of BRD4 in a dose-dependent manner in HEK293T cells[1].
PROTAC BRD4 Degrader-38 (5 μM; 2 h) covalently binds to a specific cysteine residue, particularly the C232 site, of the TRIM28 protein in HEK293T cells[1].
PROTAC BRD4 Degrader-38 (0.25 μM; 16 h) loses its ability to degrade BRD4 protein in HEK293T cells expressing the TRIM28 C232A mutant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T, HEK293T (shTRIM28), HEK293T (expressing TRIM28 mutants)
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Concentration:0.1, 0.25, 0.5, 1, 2 μM
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Incubation Time:16 h
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Result:Significantly degraded both long and short isoforms of BRD4 protein in a dose-dependent manner.
PROTAC BRD4 Degrader-38's ability to mediate BRD4 degradation was significantly attenuated in cells where the TRIM28 gene was knocked down.
Lost its ability to degrade BRD4 in cells with the C232A mutation, confirming that Cys232 is the key covalent binding site mediating degradation.
Chemical Information
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Molecular Weight 632.13
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Formula C31H30ClN7O4S
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SMILES
ClC1=CC=C(C2=N[C@@H](CC(NCCCNC(C3=CC=C(/C=C/[N+]([O-])=O)C=C3)=O)=O)C4=NN=C(C)N4C5=C2C(C)=C(C)S5)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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-38 Related Classifications
HY-175240 Related Classifications
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