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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3033545-34-2
- 分子式: C52H56ClN11O13S
- 分子量:1110.58
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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 |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3033545-34-2
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分子量 1110.58
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
phoBET1 関連分類
HY-149328 関連分類
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