2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Apoptosis Caspase Bcl-2 Family
  4. HDAC6-IN-67

HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.

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HDAC6-IN-67

HDAC6-IN-67 Chemical Structure

CAS No. : 2196247-20-6

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HDAC6-IN-67 Related Antibodies

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Description

HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer[1].

In Vitro

HDAC6-IN-67 shows significant time-dependent inhibition of tumor cells in all tested human cancer cell lines, with GI50 values ranging from 2.9 to 24.8 μM, it also shows strong anti-proliferative activity against MCF-7/ADR cells after 72 hours (GI50 = 2.4 μM)[1].
HDAC6-IN-67 (0.01-2 μM, 24 hours) can dose-dependently increase the acetylation of α-tubulin in MCF-7/ADR cells without affecting the acetylation of histone H3 even at high concentrations [1].
HDAC6-IN-67 (0.1-2 μM, 10 days) results in a significant dose-dependent inhibition of colony formation in MCF-7/ADR cells[1].
HDAC6-IN-67 (0.1-2 μM, 24 h) significantly induces early and late apoptosis, and further confirms its apoptotic effect, demonstrating a dose-dependent induction of cleavage of Caspase 9, Caspase 8, Caspase 3, and PARP, along with significant upregulation of the pro-apoptotic protein Bax and downregulation of the anti-apoptotic protein Bcl-2 in MCF-7/ADR cells[1].

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

HDAC6-IN-67 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Dose-dependently increased the acetylation of α-tubulin.
Induced α-tubulin acetylation at concentrations as low as 0.1 μM, without affecting the acetylation of Histone H3 even at concentrations up to 1 μM.

Cell Proliferation Assay[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 10 days
Result: Resulted in a significant dose-dependent inhibition of colony formation.
A concentration of 1 μM was able to suppress colony formation by approximately 65 %.

Western Blot Analysis[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Significantly induces early and late apoptosis by 25.4% and 15.7%.
The cleavage of Caspase 9, Caspase 8, Caspase 3, and PARP were significantly induced in a dose-dependent manner.
The apoptotic protein Bax was significantly induced, whereas the anti-apoptotic protein Bcl-2 was remarkably decreased in a dose-dependent manner.
In Vivo

HDAC6-IN-67 (5 mg/kg, 10 mg/kg, i.p., daily during weekdays, followed by weekend rest for 17 days) inhibits HCT116 tumor growth in vivo in a dose-dependent manner without showing significant toxicity in mice[1].

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

Animal Model: Subcutaneously injecting nude mice with HCT116 human colon cancer cells (2.0 × 106 cells/ mice).
Dosage: 5 mg/kg, 10 mg/kg
Administration: I.p., daily during weekdays, followed by weekend rest for 17 days
Result: Showed delayed tumor growth starting right after the first measurement.
Found no differences in body weight, treatment-related deaths, or abnormal behaviors between the control and experimental groups.
Molecular Weight

309.32

Formula

C17H15N3O3
CAS No.
SMILES

CC1=NC2=C(C(N1CC3=CC=C(C=C3)C(NO)=O)=O)C=CC=C2
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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HDAC6-IN-67 Related Classifications

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  • 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-672196247-20-6HDACMicrotubule/TubulinApoptosisCaspaseBcl-2 FamilyHistone deacetylasesAnticancer drugEpigeneticsHDAC6InhibitorsQuinazolin-4-oneInhibitorinhibitorinhibit

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