1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. 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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ZWZH-21

ZWZH-21 Chemical Structure

CAS No. : 3069195-42-9

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Description

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[1].

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.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.4, 0.8, and 1.6 μM
Incubation Time: 48 h
Result: Reduced HDAC1 and HDAC2 protein and increased Ac–H3 and Ac–H4 levels.

Apoptosis Analysis[1]

Cell Line: HCT116 cells and SW480 cells
Concentration: 0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
Incubation Time: 48 h
Result: Significantly increased the proportion of Annexin V-positive cells.
Showed highest apoptotic rates reaching 60.7 % and 40.04 % at low concentrations.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells and SW480 cells
Concentration: 0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
Incubation Time: 24 h
Result: Demonstrated a dose-dependent accumulation of cells in G1 phase.
In Vivo

ZWZH-21 (2000 mg/kg, orally once) shows a good safety in mice[1].
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.

Animal Model: Mice bearing HCT116 human colon cancer xenografts[1]
Dosage: 30, 60 and 120 mg/kg
Administration: Oral gavage, daily for 14 days
Result: Showed no significant body weight changes.
Suppressed tumor growth.
Molecular Weight

422.48

Formula

C26H22N4O2

CAS No.
SMILES

O=C(NC1=C(N)C=CC=C1)C2=CC=C(OCCN3C(C=NC=C4)=C4C5=C3C=CC=C5)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ZWZH-21
Cat. No.:
HY-175513
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