J-1063
J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.
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- CAS No.: 2374772-46-8
- Formule: C24H19N5OS
- Masse moléculaire:425.51
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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
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Activité biologique
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ALK5 |
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
0.039 μM
Compound: 20a; J-1063
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Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
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[PMID: 31299584] |
J-1063 (compound 4) (10 mM) shows significant ALK5 inhibitory activity (IC50s of 8.12 and 0.039 µM for p38α MAP kinase and ALK5, respectively)[1].
J-1063 (2.5, 5, 10 µM; 1 h) improved fibroblast differentiation induced by TGF-β in LX-2 cells[1].
J-1063 (2.5, 5, 10 µM; 1 h) inhibits the inflammatory response induced by TGF-β[1].
J-1063 inhibits liver fibrosis by regulating TGF-β/Smad signaling and inhibits the activation of NLPR3-Caspase-1 inflammasome[1].
J-1063 (12.5 mg/kg; Cxcl1, Cxcl2 cells) inhibits the infiltration of macrophages and neutrophils during liver fibrosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LX-2 cells
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Concentration:2.5, 5, 10 µM
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Incubation Time:1 h
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Result:Inhibited the inflammatory response induced by TGF-β.
J-1063 (12.5 mg/kg; p.o., daily for two consecutive weeks) shows benefit for TAA-induced liver fibrosis in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:i.g., one time per day, two weeks
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Result:Showed no toxic side effects on mice at low dose and was suitable for therapeutic administration.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:12.5 mg/kg
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Administration:p.o., daily for two consecutive weeks
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Result:Showed benefit for TAA-induced liver fibrosis in mice.
Chemical Information
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CAS No. 2374772-46-8
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Masse moléculaire 425.51
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Formule C24H19N5OS
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SMILES
CC1=NC(C2=NN(C=C2C3=CC4=C(S3)C=CN=C4)CC(NC5=CC=CC=C5)=O)=CC=C1
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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)
J-1063 Related Classifications
HY-145855 Related Classifications
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