HDAC6-IN-44
HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis.
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- Fòrmula: C20H21N3O3
- Peso molecular:351.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC6 8.97 nM (IC50) |
HDAC1 878 nM (IC50) |
HDAC2 3144 nM (IC50) |
HDAC4 847 nM (IC50) |
HDAC7 894 nM (IC50) |
HDAC10 1319 nM (IC50) |
HDAC11 >5000 nM (IC50) |
In Vitro
HDAC6-IN-44 (compound H10) (2.5-10 μM, 1-300 μM, 48 h) inhibits TGF-β-induced proliferation of HELF cells, cell proliferation and their HDAC6 activity in a dose-dependent manner without causing significant cytotoxic effects[1].
HDAC6-IN-44 interferes with the TGF-β1-related fibrosis process by acting on HDAC6-related signaling pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HELF cells
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Concentration:2.5-10 μM (cell proliferation test), 1-300 μM (survival toxicity test)
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Incubation Time:48 h
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Result:Inhibited TGF-β-induced HELF cell proliferation without significantly inhibiting cell survival at a maximum concentration of approximately 10 μM.
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Cell Line:HELF cells
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Concentration:2.5-10 μM
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Incubation Time:48 h
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Result:Exhibited dose-dependent increase in acetylated α-tubulin expression and has no effect on histone H3 acetylation, while attenuating the elevated expression of all marker proteins induced by TGF-β1.
In Vivo
HDAC6-IN-44 (0.1 mL/10g, i.p., daily for 3 weeks) can inhibit the progression of pulmonary fibrosis in a dose-dependent manner in a mouse model of pulmonary fibrosis[1].
Cell Viability Assay[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin-induced pulmonary fibrosis mouse model[1]
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Dosage:0.1 mL/10g
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Administration:Intraperitoneal injection (i.p.) , daily for 3 weeks
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Result:Caused the blue collagen fiber deposition to be spot-like, with the surrounding alveolar cavity slightly collapsed and the alveolar wall thickened, but the collagen fiber deposition was significantly less than that in the model group. Additionally, HDAC6-IN-44 could dose-dependently inhibit the expression of α-SMA and p-Smad2/3 in BLM-induced pulmonary fibrosis in mice.
Chemical Information
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Peso molecular 351.40
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Fòrmula C20H21N3O3
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SMILES
O=C(NO)C1=CC=C(CN2C([C@@](CCC3)([H])N3CC4=CC=CC=C42)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC6-IN-44 Related Classifications
HY-162630 Related Classifications
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