2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. HDAC Apoptosis Pyroptosis Reactive Oxygen Species (ROS) Caspase
  4. HDAC1/6-IN-3

HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.

For research use only. We do not sell to patients.

HDAC1/6-IN-3

HDAC1/6-IN-3 Chemical Structure

CAS No. : 3038691-85-6

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HDAC1/6-IN-3 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer[1].

IC50 & Target[1]

HDAC1

1.1 nM (IC50)

HDAC6

2.7 nM (IC50)

In Vitro

HDAC1/6-IN-3 (Compound 15a) (72 h)shows excellent inhibitory activities against HepG2 (IC50 = 0.12 μM), PC9 (IC50 = 0.53 μM), HCT116 (IC50 = 1.12 μM) and MCF7 cell (IC50 = 3.12 μM)[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) increases the level of acetyl-H3 and H4 in a dose-dependent manner in HepG2 cells[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 10-14 d) suppresses the formation of colonies of HepG2 cells in a dose-dependent manner.[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) induces G0/G1 arrest in HepG2 cells may be correlated the downregulation of with CDK4 and Cyclin D1 proteins[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 48 h) enhances ROS generation and DNA damage accumulation to induce apoptosis in HepG2 cells[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24-48 h) triggers pyroptosis in HepG2 cells through caspase-3 cleavage of GSDME[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC1/6-IN-3 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Significantly inhibited HepG2 cells in G0/G1 phase in a dose-dependent manner.
The G2/M ratio decreased from 25.34 to 22.85% and the S-phase value decreased from 32.99 to 13.72%.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 48 h
Result: Induced apoptosis in 28.2% at 0.2 µM and 46.5% at 0.5 µM.

Immunofluorescence[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Dose-dependently increased the ROS levels.
Showed dose-dependent γH2AX foci formation.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Increased the levels of acetyl-H3 and H4 in a dose-dependent manner.
Down-regulated the expression of Cyclin D1 and CDK4.
Upregulated the expression of Cl-PARP, Cl-caspase 3 in a dose-dependent manner.
Resulted in elevated levels of the N-terminal fragment of gasdermin E (GSDME) and caspase-3.
In Vivo

HDAC1/6-IN-3 (Compound 15a) (10 mg/kg, i.p., twice a week for 3 weeks) shows the significant antitumor efficacy in HepG2 xenograft model, coupled with an acceptable safety profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HepG2 induced xenograft model established in male BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week for 3 weeks
Result: Dose-dependently inhibited the growth of tumors.
Observed a dose-dependent reduction in Ki67 immunostaining.
Induced the increase of Ac- H3/H4､Cl-caspase3 and GSDME-N in a dose-dependent manner.
Molecular Weight

453.55

Formula

C24H27N3O4S
CAS No.
SMILES

O=C(NO)CCCCCC(N(C1=CC=C(OC)C=C1)CC2=CSC(C3=CC=CC=C3)=N2)=O
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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HDAC1/6-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

HDAC1/6-IN-33038691-85-6HDACApoptosisPyroptosisReactive Oxygen Species (ROS)CaspaseHistone deacetylasesHistone deacetylase inhibitorThiazoleHydroxamateAnticancerHepG2 cellsInhibitorinhibitorinhibit

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