2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-47

HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.

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HDAC-IN-47 Chemical Structure

HDAC-IN-47 Chemical Structure

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HDAC-IN-47 Related Antibodies

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Description

HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo[1].

IC50 & Target[1]

HDAC1

19.75 nM (IC50)

HDAC6

5.63 nM (IC50)

HDAC3

40.27 nM (IC50)

HDAC2

57.8 nM (IC50)

HDAC8

302.73 nM (IC50)

In Vitro

HDAC-IN-47 (compound 21) shows antiproliferative activity and inhibits A549 cell growth with an IC50 value of 0.24 μM[1].
HDAC-IN-47 (0.5 and 1 μM; 72 h) exhibits profound G2/M arrest in A549 cells and induces cell apoptosis[1].
HDAC-IN-47 (0.1 and 0.5 μM; 24 h) increases the expression levels of Bax and Caspase3, decreases the level of Bcl-2, activates the intrinsic (mitochondrial) apoptotic pathway[1].

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

HDAC-IN-47 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2, MDA-MB-238, HL-60 cells
Concentration: 0.16-0.45 μM
Incubation Time: 72 hours
Result: Inhibited cancer cells with IC50s of 0.16 μM (HepG2), 0.45 μM (MDA-MB-238), 0.22 μM (HL-60), respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Induced marked arrest of cells in the G2/M phase of 28.38% (0.5 μM) and 31.70% (1.0 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Resulted 21.09% (0.5 μM) and 30.58% (1 μM) apoptotic cells.
In Vivo

HDAC-IN-47 (compound 21) (50, and 100 mg/kg; p.o.; once daily; 18 d) exhibits significant antitumor activity in a dosedependent manner without no significant body weight loss in A549 xenograft mouse model[1].

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

Animal Model: A549 xenograft model in mouse (female, BALB/c nu/nu mice, 6-8 weeks old)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: Oral gavage; once daily; for 18 consecutive days
Result: Decreased the tumor volume and weight by 48% and 45%, respectively.
Molecular Weight

410.26

Formula

C17H20BrN3O4
SMILES

O=C(C1=NC=C(C2=CC=C(Br)C=C2)O1)NCCCCCCC(NO)=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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HDAC-IN-47 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:

HDAC-IN-47HDACHistone deacetylasesantiproliferativeanti-tumorarrests cell cycleG2/MHepG2MDA-MB-238HL-60A549Inhibitorinhibitorinhibit

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