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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- CAS No.: 3033545-34-2
- Formule: C52H56ClN11O13S
- Masse moléculaire:1110.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
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.
|
37279091 |
In Vitro
phoBET1 loses the CRBN recruitment ability due to the steric hindrance of its caging group, exhibits no BRD4 degradation activity in MV-4-11 cells, but restores this activity after activation by 365 nm UV light[1].
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].
phoBET1 can be rapidly photolyzed by 365 nm ultraviolet light to release active dBET1 (HY-101838) in a time-dependent manner, while remaining stable under 980 nm near-infrared light[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.
Chemical Information
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CAS No. 3033545-34-2
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Masse moléculaire 1110.58
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
phoBET1 Related Classifications
HY-149328 Related Classifications
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