2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC6-IN-4

HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity.

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HDAC6-IN-4 Chemical Structure

HDAC6-IN-4 Chemical Structure

CAS No. : 2709103-20-6

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HDAC6-IN-4 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-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1].

IC50 & Target

HDAC6

23 nM (IC50)

HDAC3

46 nM (IC50)

HDAC2

172 nM (IC50)

HDAC8

2175 nM (IC50)

HDAC1

3604 nM (IC50)

In Vitro

HDAC6-IN-4 (C10) (0-50 µM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity[1].
HDAC6-IN-4 (0-6 µM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1[1].
HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells[1].
HDAC6-IN-4 (0-8 µM, 24 h) induces B16 cell apoptosis in a dose-dependent manner[1].
HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes[1].

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

HDAC6-IN-4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: B16, HepG2, A549, and CT26 cells
Concentration: 0-50 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50 values of 1.52, 2.36, 5.77, and 2.09 µM against B16, HepG2, A549, and CT26 cells, respectively.

Western Blot Analysis[1]

Cell Line: B16 and CT26 cancer cells
Concentration: 2, 4, and 6 µM
Incubation Time: 2, 4, 8, 12, and 24 h
Result: Dramatically increased the level of Ac-Tub (acetyl-α-tubulin) in a dose-dependent and time-dependent manner. Had almost no effect on the content of Ac-H3 (acetyl-H3).

Apoptosis Analysis[1]

Cell Line: B16 cells
Concentration: 4, 6, and 8 µM
Incubation Time: 24 h
Result: Caused moderate to potent induction of apoptosis in the B16 cell line in a dose-dependent manner. Upregulated the expression of apoptotic protein cleaved PARP.
In Vivo

HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity[1].

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

Animal Model: Five-week-old C57BL/6 mice (immune-related CT26 xenograft model)[1].
Dosage: 50 and 100 mg/kg
Administration: Oral gavage, once daily for 21 days
Result: Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity.
Molecular Weight

506.63

Formula

C30H38N2O5
CAS No.
SMILES

O=C(NO)CCCCCCNCC1=C(OC)C=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OC
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-4 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-42709103-20-6HDACApoptosisHistone deacetylasesB16HepG2A549CT26Ac-TubIFN-gT cellHDAC2HDAC3Inhibitorinhibitorinhibit

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