MHY219
MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer.
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- CAS No.: 1326750-61-1
- Formule: C20H25N3O3
- Masse moléculaire:355.43
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Stockage:
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
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Activité biologique
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Chemical Information
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Activité biologique
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Bax |
Bcl-2 |
MHY219 (0.001-10 μM; 30 min) potently inhibits total HDAC enzyme activity with an IC50 of 0.276 μM in a cell-free fluorometric assay[1].
MHY219 (0.05-5 μM; 24-48 h) inhibits the proliferation of DU145, LNCaP, and PC3 human prostate cancer cells with 48 h IC50 values of 0.36 μM, 0.97 μM, and 5.12 μM, respectively, and induces morphological changes in DU145 cells[1].
MHY219 (0.1-1 μM; 48 h) increases histone H3 and H4 hyperacetylation and down-regulates specific class I and II HDAC subtypes in DU145, LNCaP, and PC3 human prostate cancer cells[1].
MHY219 (0.1-1 μM; 48 h) induces sub-G1 accumulation and G2/M phase arrest in DU145 cells, G1 phase arrest in LNCaP cells, and G2/M phase arrest in PC3 cells, with corresponding changes in cell cycle regulatory protein expression[1].
MHY219 (0.1-1 μM; 24-48 h) induces apoptosis in DU145 human prostate cancer cells via a mitochondria-mediated pathway, but does not induce apoptosis in LNCaP or PC3 cells[1].
MHY219 (0.5-1 μM; 48 h) increases androgen receptor expression in DU145 human prostate cancer cells, but does not affect AR expression in LNCaP or PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145, LNCaP, PC3 human prostate cancer cell lines
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Concentration:0.05, 0.1, 0.3，0.5, 0.8, 1, 3, 5 μM
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Incubation Time:24 h; 48 h
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Result:Reduced cell viability in a concentration-dependent manner across all three cell lines.
At 48 h, reached IC50 values of 0.36 μM for DU145 cells, 0.97 μM for LNCaP cells, and 5.12 μM for PC3 cells.
Induced cytoplasmic enlargement and cellular flattening in DU145 cells after 48 h treatment.
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Cell Line:DU145, LNCaP, PC3 human prostate cancer cell lines
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:48 h
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Result:Increased histone H3 and H4 hyperacetylation in all three cell lines; in PC3 cells, hyperacetylation of H3 was low at 0.5 μM but pronounced at 1 μM.
Down-regulated levels of all class I HDACs (1, 2, 3, 8) and most class II HDACs (except HDAC5, 6, 10) in DU145 cells.
Down-regulated HDAC1, 2, 3, and HDAC6 in LNCaP cells.
Down-regulated class I HDACs (1, 2, 3) and HDAC4 in PC3 cells.
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Cell Line:DU145, LNCaP, PC3 human prostate cancer cell lines
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:48 h
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Result:Significantly increased the sub-G1 fraction in a concentration-dependent manner, induced G2/M phase arrest, and decreased the S phase population in DU145 cells.
Induced G1 phase arrest in a concentration-dependent manner in LNCaP cells.
Induced G2/M phase arrest in PC3 cells.
Decreased cyclin A1 and cyclin B1, increased cyclin D1, and increased p21 expression in DU145 cells.
Decreased cyclin D1 and increased p21 expression in LNCaP cells.
Increased cyclin D1 without affecting p21 in PC3 cells.
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Cell Line:DU145, LNCaP, PC3 human prostate cancer cell lines
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Concentration:0.1, 0.5, 1 μM (Annexin V/PI, WB); 1 μM (DAPI staining)
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Incubation Time:24 h; 48 h (Annexin V/PI, WB); 48 h (DAPI staining)
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Result:Increased late apoptosis in a concentration-dependent manner at 48 h and increased cleavage of PARP, increased Bax and cytochrome c release, and decreased Bcl-2 expression in DU145 cells.
Showed increased condensed or fragmented chromatin (apoptotic nuclei) in DU145 cells via DAPI staining.
Did not induce apoptotic cell death in LNCaP or PC3 cells at tested concentrations.
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Cell Line:DU145, LNCaP, PC3 human prostate cancer cell lines
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Concentration:0.5, 1 μM
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Incubation Time:48 h
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Result:Markedly increased AR expression in DU145 cells.
Did not affect AR expression in LNCaP or PC3 cells.
Chemical Information
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CAS No. 1326750-61-1
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Masse moléculaire 355.43
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Formule C20H25N3O3
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SMILES
O=C(NO)CCCCCCC(NC1=CC=C(NC2=CC=CC=C2)C=C1)=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)
MHY219 Related Classifications
HY-116267 Related Classifications
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