PROTAC BRD4 Degrader-6
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research.
(Pink: BRD4 ligand (HY-100015); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-108369)).
For research use only. We do not sell to patients.
- CAS No.: 2410947-56-5
- Formula: C43H40F2N10O10S
- Molecular Weight:926.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD4 BD1 2.7 μM (IC50) |
Caspase 3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
0.165 μM
Compound: PROTAC 29
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Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition
Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition
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[PMID: 34411892] |
| BXPC-3 | IC50 |
0.17 μM
Compound: 11
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Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 36202064] |
PROTAC BRD4 Degrader-6 (compound 32a) (72 hours; BxPC3 cell) has anti-proliferation activity with IC50 value of 0.165 μM[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces BRD4 protein degradation in a time-dependent manner, which results in the continuous decrease of c-Myc expression[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces the cell cycle arrest and apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC3 cell
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Concentration:1 μM
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Incubation Time:48 hours
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Result:Degraded BRD4 protein in a time-dependent manner and inhibits the expression of c-Myc.
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Cell Line:BxPC3 cell
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Concentration:1 μM
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Incubation Time:48 hours
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Result:Increase in G0/G1 and G2/M phase cells, and a decrease of S phase cells.
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Cell Line:BxPC3 cell
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Concentration:1 μM
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Incubation Time:48 hours
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Result:The percentage of cells in early and late apoptosis was recorded as 10.10% and 12.36%, respectively.
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Cell Line:BxPC3 cell
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Concentration:1 μM
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Incubation Time:48 hours
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Result:The expression of caspase 3 and cleaved-caspase 3 significantly increased.
Chemical Information
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CAS No. 2410947-56-5
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Molecular Weight 926.90
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Formula C43H40F2N10O10S
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SMILES
O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCC5=CN(CCOCC(NC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)=O)N=N5
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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)
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