ZWZH-21
ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer.
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- CAS No.: 3069195-42-9
- Formule: C26H22N4O2
- Masse moléculaire:422.48
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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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
HDAC1 34 nM (IC50) |
HDAC2 41 nM (IC50) |
HDAC3 277 nM (IC50) |
HDAC6 >800 nM (IC50) |
HDAC8 >800 (IC50) |
In Vitro
ZWZH-21 inhibits A549, MCF-7 and HepG2 cells growth with IC50 values of 1.66 μM, 2.445 and 1.551 μM, respectively[1].
ZWZH-21 (1 μM, 6 h) inhibits temperature-induced HDAC1/2 degradation in HCT116 cells[1].
ZWZH-21 (0.4-1.6 μM, 48 h) induces the degradation of HDAC1 and HDAC2 protein and the formation of Ac–H3 and histone H4 in a concentration-dependent manner in HCT116 cells[1].
ZWZH-21 (0.4-1.6 μM, 48 h) inhibits the colony-forming ability in HCT116 and SW480 cells[1].
ZWZH-21 (0.4-2 μM, 48 h) suppresses cell migration and induces apoptosis in HCT116 and SW480 cells[1].
ZWZH-21 (0.4-2 μM, 24 h) induces G1 phase arrest in HCT116 and SW480 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 cells
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Concentration:0.4, 0.8, and 1.6 μM
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Incubation Time:48 h
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Result:Reduced HDAC1 and HDAC2 protein and increased Ac–H3 and Ac–H4 levels.
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Cell Line:HCT116 cells and SW480 cells
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Concentration:0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
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Incubation Time:48 h
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Result:Significantly increased the proportion of Annexin V-positive cells.
Showed highest apoptotic rates reaching 60.7 % and 40.04 % at low concentrations.
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Cell Line:HCT116 cells and SW480 cells
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Concentration:0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
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Incubation Time:24 h
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Result:Demonstrated a dose-dependent accumulation of cells in G1 phase.
In Vivo
ZWZH-21 (30-120 mg/kg, i.g., daily for 14 days) suppresses tumor growth in mice bearing HCT116 human colon cancer xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing HCT116 human colon cancer xenografts[1]
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Dosage:30, 60 and 120 mg/kg
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Administration:Oral gavage, daily for 14 days
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Result:Showed no significant body weight changes.
Suppressed tumor growth.
Chemical Information
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CAS No. 3069195-42-9
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Masse moléculaire 422.48
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Formule C26H22N4O2
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SMILES
O=C(NC1=C(N)C=CC=C1)C2=CC=C(OCCN3C(C=NC=C4)=C4C5=C3C=CC=C5)C=C2
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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)
ZWZH-21 Related Classifications
HY-175513 Related Classifications
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