phoBET1
phoBET1 is a photolabile PROTAC molecule that, upon photoactivation, functions as a BRD4 PROTAC degrader to trigger BRD4 degradation via the ubiquitin-proteasome system. Activated phoBET1 induces cancer cell apoptosis and inhibits tumor growth in xenograft mouse models. In its inactive caged state, phoBET1 exhibits only extremely low antiproliferative activity against cancer cells. phoBET1 can be applied in studies related to acute myeloid leukemia.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker).
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- No. CAS: 3033545-34-2
- Fòrmula: C52H56ClN11O13S
- Peso molecular:1110.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRD4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
114.2 nM
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Antiproliferative activity against human MV-4-11 leukemia cells after pre-incubation with phoBET1 for 2 h, exposure to 365 nm UV light for 5 min, and further incubation, measured by Cell Counting Kit-8 (CCK8) assay.
Antiproliferative activity against human MV-4-11 leukemia cells after pre-incubation with phoBET1 for 2 h, exposure to 365 nm UV light for 5 min, and further incubation, measured by Cell Counting Kit-8 (CCK8) assay.
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37279091 |
In Vitro
phoBET1 alone exhibits only extremely low antiproliferative activity against MV-4-11 cells, but upon activation with 365 nm UV light, it displays potent antiproliferative activity with an IC50 of 114.2 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 3033545-34-2
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Peso molecular 1110.58
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Fòrmula C52H56ClN11O13S
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SMILES
COC1=CC(C(OCN(C(CCC2N3C(C4=CC=CC(OCC(NCCCCNC(C[C@H]5C6=NN=C(N6C7=C(C(C8=CC=C(C=C8)Cl)=N5)C(C)=C(C)S7)C)=O)=O)=C4C3=O)=O)=O)C2=O)C)=C(C=C1OCC(NCCN)=O)[N+]([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
phoBET1 Related Classifications
HY-149328 Related Classifications
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