JPS004
JPS004 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3. JPS004 induces extensive transcriptomic changes in human colon cancer cell line HCT116, including downregulation of HDAC complex components and cell cycle regulatory machinery, modulation of the AKT/mTOR signaling pathway, and upregulation of FOXO-mediated apoptosis and autophagy related genes. JPS004 can be used in colon cancer-related research.
(Pink: ligand (HY-50934); Blue: ligand (HY-125845); Black: linker).
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- CAS 番号: 2559747-12-3
- 分子式: C47H61N7O6S
- 分子量:852.10
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
HDAC1 |
HDAC2 |
HDAC3 |
mTORC2 |
mTORC1 |
Akt |
mTOR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
4.3 μM
Compound: 1; JPS004
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Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
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[PMID: 35293758] |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced degradation of HDAC1, HDAC2, and HDAC3, with a slight preference for HDAC1/2 degradation over HDAC3.
Produced increases in histone acetylation levels at H3K56 (H3K56ac) and H2BK5 (H2BK5ac), though these increases were smaller than those induced by CI-994 treatment.
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Cell Line:HCT116 human colon cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced cell viability, with 33% of cells in the sub-G1 (cell death) population and 67% live cells, compared to 95% live cells in DMSO-treated controls.
Induced alterations in cell cycle distribution relative to untreated controls.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Autophagy
- Apoptosis Solutions
- Protocol for Cell Cycle
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
化学情報
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CAS 番号 2559747-12-3
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分子量 852.10
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分子式 C47H61N7O6S
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SMILES
NC(C=CC=C1)=C1NC(C(C=C2)=CC=C2NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)=O)=O)=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)
JPS004 関連分類
HY-176904 関連分類
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Keywords
- JPS004
- 2559747-12-3
- JPS 004
- JPS-004
- PROTACs
- HDAC
- FOXO
- mTOR
- Akt
- Apoptosis
- Autophagy
- PROTAC
- Histone deacetylases
- Forkhead box O
- Mammalian target of Rapamycin
- PKB
- Protein kinase B
- colon carcinoma
- HCT116 human colon cancer cells
- colon cancer
- proteasome
- HDAC2
- VHL E3 ubiquitin ligase
- HDAC1
- histone acetylation
- FOXO3
- HDAC3
- Inhibitor
- inhibitor
- inhibit