1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. J-1063

J-1063 

Cat. No.: HY-145855
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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.

For research use only. We do not sell to patients.

J-1063 Chemical Structure

J-1063 Chemical Structure

CAS No. : 2374772-46-8

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Description

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[1].

IC50 & Target

IC50: 0.039 µM (ALK5)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: LX-2 cells
Concentration: 2.5, 5, 10 µM
Incubation Time: 1 h
Result: Inhibited the inflammatory response induced by TGF-β.
In Vivo

J-1063 (12.5, 25, 50 mg/kg; i.g., one time per day for two weeks) shows no toxic side effects on mice at low dose and is suitable for therapeutic administration[1].
J-1063 (12.5 mg/kg; p.o., daily for two consecutive weeks) shows benefit for TAA-induced liver fibrosis in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: i.g., one time per day, two weeks
Result: Showed no toxic side effects on mice at low dose and was suitable for therapeutic administration.
Animal Model: Male C57BL/6 mice[1]
Dosage: 12.5 mg/kg
Administration: p.o., daily for two consecutive weeks
Result: Showed benefit for TAA-induced liver fibrosis in mice.
Molecular Weight

425.51

Formula

C24H19N5OS

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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J-1063
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