PROTAC BRD4 Degrader-36
PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader with a DC50 of 0.649 nM. It has a Kd of 123 nM for TRIM21. PROTAC BRD4 Degrader-36 recruits the E3 ubiquitin ligase TRIM21 (Kd = 123 nM) to BRD4, leading to ubiquitination and subsequent degradation of BRD4. PROTAC BRD4 Degrader-36 exhibits cytotoxicity against PANC-1 cells (GI50 = 0.103 μM). It can be used in research related to pancreatic cancer.
(Pink: BRD4 ligand (HY-129939); Blue: TRIM21 ligand (HY-175241); Black: linker).
For research use only. We do not sell to patients.
- Formula: C52H58F2N6O7S3
- Molecular Weight:1013.24
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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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Biological Activity
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BRD4 0.649 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | DC50 |
0.649 nM
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BRD4 degradation in human PANC-1 cells assessed via high-content analysis (HCA) after 24 hours of incubation.
BRD4 degradation in human PANC-1 cells assessed via high-content analysis (HCA) after 24 hours of incubation.
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40623734 |
| PANC-1 | GI50 |
0.103 μM
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Antiproliferative activity against human PANC-1 cells assessed via antiproliferation assay.
Antiproliferative activity against human PANC-1 cells assessed via antiproliferation assay.
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40623734 |
PROTAC BRD4 Degrader-36 (Compound TrimTAC-1) (0.001-10 μM; 3 days) inhibits the proliferation of PANC-1 cells, with a GI50 value of 0.103 μM[1].
PROTAC BRD4 Degrader-36 (0.01 nM-10 mM; 24 h) exerts a dose-dependent BRD4 protein degradation effect in PANC-1 cells, with a DC50 of 0.649 nM and a Dmax of 71%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1013.24
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Formula C52H58F2N6O7S3
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SMILES
O=C(C1=C(C=C2C3=CN(C(C4=C3C(CN(C2=C1)C5=NC=C(C=C5F)F)=CN4)=O)C)CS(C)(=O)=O)NCCCCCCCN(CC6CCCCC6)C(C7=C(S(=O)(C)=O)C=C(C=C7)C8=CC=CC=C8SC)=O
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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-36 Related Classifications
HY-175224 Related Classifications
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