HDAC-IN-45
HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
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- CAS No.: 2421122-61-2
- Formule: C25H20ClFN8O
- Masse moléculaire:502.93
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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HDAC1 0.108 μM (IC50) |
HDAC2 0.585 μM (IC50) |
HDAC3 0.563 μM μM (IC50) |
HDAC6 ﹥10 μM (IC50) |
HDAC8 6.81 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
2.44 μM
Compound: 14
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Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32325365] |
| MDA-MB-231 | IC50 |
1.48 μM
Compound: 14
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32325365] |
HDAC-IN-45 (Compound 14) suppresses the growth of triple-negative breast cancer cells MDA-MB-231 (IC50 = 1.48 μM), MDA-MB-468 (IC50= 0.65 μM), and liver cancer cells HepG2 (IC50= 2.44 μM).
HDAC-IN-45 has equally virulent in the HDAC-sensitive cell lines (YCC11) and -resistant gastric cell lines (YCC3/7) and overcome HDACi resistance. HDAC-IN-45 has a high toxicity (IC50= 0.33 μM) in three leukemic cell lines, K-562, KG-1 and THP-1.
HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
HDAC-IN-45 (Compound 14) can elevate acetylation level of histone H3 and expression of p21.
HDAC-IN-45 (Compound 14) exerts a dose-dependent upregulation of ac-H3K9 in MDA-MB-231 cells, triggers cell cycle arrest in G1 phase.
HDAC-IN-45 (Compound 14) exhibits a potent antitumor efficacy in xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Triple-negative breast cancer cells; liver cancer cells; YCC11 and YCC3/7
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Concentration:a series of concentration
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Incubation Time:72 h
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Result:Inhibited the cell growth viability of HepG2 and triple-negative breast cancer cells.
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Cell Line:Three leukemic cell lines (K-562, KG-1 and THP-1); YCC3/7 and YCC11 cell lines
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Concentration:a series of concentration
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Incubation Time:72 h
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Result:Showed a potent anti-cancer effect, exhibited high sensitivities and strong toxicities with IC50 values below micromolar in leukemic cell lines.
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Cell Line:MDA-MB-231 cells
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Concentration:2 µM
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Incubation Time:24 h
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Result:Elevated acetylation level of histone H3 and expression of p21.
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Cell Line:MDA-MB-231cells
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Concentration:4 µM
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Incubation Time:24 h
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Result:Arrested cell cycle in G1 and trigger apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human MDA-MB-231 breast cancer xenograft mouse model[1]
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Dosage:25 mg/kg or 50mg/kg
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Administration:25 mg/kg or 50mg/kg; i.p.; every day.
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Result:Exhibited a potent antitumor efficacy.
Chemical Information
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CAS No. 2421122-61-2
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Masse moléculaire 502.93
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Formule C25H20ClFN8O
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SMILES
O=C(NC1=CC=CC=C1N)C2=CC=C(CN3C=NC4=C(NC5=CC=C(F)C(Cl)=C5)N=C(N)N=C34)C=C2
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-45 Related Classifications
HY-150577 Related Classifications
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