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

HDAC-IN-47 Chemical Structure

CAS No. : 3033608-94-2

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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)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.24 μM
Compound: 21
Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
HL-60 IC50
0.22 μM
Compound: 21
Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
HepG2 IC50
0.16 μM
Compound: 21
Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
MDA-MB-238 IC50
0.45 μM
Compound: 21
Anticancer activity against human MDA-MB-238 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human MDA-MB-238 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
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
CAS No.
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-473033608-94-2HDACHistone deacetylasesantiproliferativeanti-tumorarrests cell cycleG2/MHepG2MDA-MB-238HL-60A549Inhibitorinhibitorinhibit

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