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: HDAC1-3 ligand (HY-50934); Blue: VHL ligand (HY-125845); Black: linker).
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- No. CAS: 2559747-12-3
- Fòrmula: C47H61N7O6S
- Peso molecular:852.10
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
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 |
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| 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] |
In Vitro
JPS004 (10 μM; 24 h) degrades HDAC1, HDAC2, and HDAC3 and increases H3K56ac and H2BK5ac levels in HCT116 human colon cancer cells[1].
JPS004 (10 μM; 24 h) reduces viability and alters cell cycle distribution in HCT116 human colon cancer cells[1].
JPS004 (10 μM; 24 h) induces widespread transcriptomic changes, including downregulation of HDAC complex components and cell cycle machinery, modulation of AKT/mTOR signaling, and upregulation of FOXO-driven apoptosis and autophagy genes, in HCT116 human colon cancer cells[1].
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
Chemical Information
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No. CAS 2559747-12-3
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Peso molecular 852.10
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Fòrmula 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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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)
JPS004 Related Classifications
HY-176904 Related Classifications
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