2. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  3. HDAC Apoptosis PERK Microtubule/Tubulin
  4. HDAC6-IN-74

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.

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

HDAC6-IN-74

HDAC6-IN-74 Chemical Structure

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HDAC6-IN-74 Related Antibodies

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

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Description

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer[1].

IC50 & Target[1]

HDAC6

0.036 μM (IC50)

HDAC1

3.0 μM (IC50)

HDAC2

2.3 μM (IC50)

HDAC3

4.9 μM (IC50)

HDAC4

2.1 μM (IC50)

HDAC5

8.4 μM (IC50)

HDAC10

1.7 μM (IC50)

HDAC11

6.4 μM (IC50)

In Vitro

HDAC6-IN-74 (compound 14a) (0.05-50.0 μM; 72 h) potently inhibits the proliferation of HepG2 hepatocellular carcinoma cells with an IC50 of 0.7 μM, shows low activity against Huh7 cells, exhibits no activity against LM3 cells, and has high selectivity for tumor cells relative to non-tumorigenic cell lines[1].
HDAC6-IN-74 (1-10 μM; 0-72 h) induces apoptosis and S-phase cell cycle arrest, and inhibits cell invasion and migration in HepG2 cells[1].
HDAC6-IN-74 (0-10.0 μM; 24 h) downregulates the expressions of HDAC6 and p-ERK1/2, and upregulates the expressions of Ac-H3 and Ac-α-tubulin in HepG2 cells[1].

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

HDAC6-IN-74 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HepG2, Huh7, LM3, THLE-2
Concentration: 50.0, 25.0, 10.0, 5.0, 2.5, 1.0, 0.5, 0.1 and 0.05 μM
Incubation Time: 72 h
Result: Exhibited an IC50 of 0.7 μM against HepG2 cells, 9.4 μM against Huh7 cells, >50 μM against LM3 cells, >50 μM against THLE-2 cells.

Apoptosis Analysis[1]

Cell Line: HepG2
Concentration: 1 μM, 10 μM
Incubation Time: 72 h
Result: Induced an apoptotic rate of 19.48% at 1 μM.
Induced an apoptotic rate of 25.73% at 10 μM.

Western Blot Analysis[1]

Cell Line: HepG2
Concentration: 0, 0.5, 1.0, 2.5, 5.0 and 10.0 μM
Incubation Time: 24 h
Result: Significantly reduced HDAC6 and p-ERK1/2 protein levels at 2.5 μM.
Dose-dependently increased Ac-H3 and Ac-α-tubulin protein levels without affecting total H3 or α-tubulin levels at concentrations from 0.5 to 10.0 μM.
In Vivo

HDAC6-IN-74 (12.5-25.0 mg/kg; intragastric administration; once every other day; 24 days) exhibits potent dose-dependent in vivo anti-tumor activity against xenograft tumors[1].

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

Animal Model: BALB/c nude mice treated HepG2 (female, 6-week-old)[1]
Dosage: 12.5 mg/kg; 25.0 mg/kg
Administration: Intragastric administration.; every other day; 24 days
Result: Achieved a 47.6% tumor inhibition rate, significantly reduced HDAC6 protein levels in tumor tissue, significantly increased Ac-α-tubulin protein levels in tumor tissue, and induced tumor cell apoptosis at 12.5 mg/kg.
Achieved a 90.2% tumor inhibition rate, caused a more significant reduction in HDAC6 protein levels in tumor tissue compared to the 12.5 mg/kg dose, increased Ac-α-tubulin protein levels to ~15.4-fold that of the control group, and induced the highest level of tumor cell apoptosis among the treatment groups at 25 mg/kg.
Caused no obvious changes in mouse body weight or histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney).
Molecular Weight

378.35

Formula

C16H17N3OSSe
SMILES

O=C(NC1=NC=C(C2=CC=CC=C2)S1)CCCCC[Se]C#N
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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HDAC6-IN-74 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:

HDAC6-IN-74HDACApoptosisPERKMicrotubule/TubulinHistone deacetylasesProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasehepatocellular carcinomacell migrationhistone deacetylase 6apoptosisERK1/2HepG2Huh7HDAC6cell invasionInhibitorinhibitorinhibit

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