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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2374772-46-8
- Formel: C24H19N5OS
- Molecular Weight:425.51
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
|
ALK5 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.039 μM
Compound: 20a; J-1063
|
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
|
[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.
-
Cell Line:LX-2 cells
-
Concentration:2.5, 5, 10 µM
-
Incubation Time:1 h
-
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.
-
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.
Chemical Information
-
CAS. Nr. 2374772-46-8
-
Molecular Weight 425.51
-
Formel C24H19N5OS
-
SMILES
CC1=NC(C2=NN(C=C2C3=CC4=C(S3)C=CN=C4)CC(NC5=CC=CC=C5)=O)=CC=C1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
J-1063 Related Classifications
HY-145855 Related Classifications
Powered by Bioz