HDAC-IN-47
Based on 1 publication(s) in Google Scholar
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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- CAS No.: 3033608-94-2
- Formule: C17H20BrN3O4
- Masse moléculaire:410.26
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) HDAC-IN-47
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Activité biologique
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.24 μM
Compound: 21
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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
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[PMID: 36215854] |
| HepG2 | IC50 |
0.16 μM
Compound: 21
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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
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[PMID: 36215854] |
| HL-60 | IC50 |
0.22 μM
Compound: 21
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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
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[PMID: 36215854] |
| MDA-MB-238 | IC50 |
0.45 μM
Compound: 21
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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
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[PMID: 36215854] |
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.
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Cell Line:HepG2, MDA-MB-238, HL-60 cells
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Concentration:0.16-0.45 μM
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Incubation Time:72 hours
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Result:Inhibited cancer cells with IC50s of 0.16 μM (HepG2), 0.45 μM (MDA-MB-238), 0.22 μM (HL-60), respectively.
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Cell Line:A549 cells
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Concentration:0.5 and 1 μM
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Incubation Time:24 hours
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Result:Induced marked arrest of cells in the G2/M phase of 28.38% (0.5 μM) and 31.70% (1.0 μM).
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Cell Line:A549 cells
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Concentration:0.5 and 1 μM
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Incubation Time:24 hours
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Result:Resulted 21.09% (0.5 μM) and 30.58% (1 μM) apoptotic cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft model in mouse (female, BALB/c nu/nu mice, 6-8 weeks old)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:Oral gavage; once daily; for 18 consecutive days
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Result:Decreased the tumor volume and weight by 48% and 45%, respectively.
Chemical Information
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CAS No. 3033608-94-2
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Masse moléculaire 410.26
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Formule C17H20BrN3O4
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SMILES
O=C(C1=NC=C(C2=CC=C(Br)C=C2)O1)NCCCCCCC(NO)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Pureté et documentation
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-47 Related Classifications
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