Application | Comment | Organism |
---|---|---|
medicine | potential for activin receptor-like kinase-5 inhibition in prevention and progression of disease, inhibition of activin receptor-like kinase-5 signaling in vivo with the selective small-molecule inhibitor IN-1233 prevented pulmonary arterial hypertension, right ventricular hypertrophy, and vascular remodeling after monocrotaline injection and inhibited the progression of established pulmonary arterial hypertension in this model | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)benzamide | IN-1233, inhibitor specifically inhibits TGF-beta signaling via ALK-5 by acting as a competitive inhibitor of the ATP-binding site, inhibition of activin receptor-like kinase-5 signaling in vivo with the selective small-molecule inhibitor prevents pulmonary arterial hypertension, right ventricular hypertrophy, and vascular remodeling after monocrotaline injection and inhibits the progression of established pulmonary arterial hypertension in this model | Rattus norvegicus | |
SD-208 | inhibitor reduces the monocrotaline-induced increase in RV systolic pressure, but the effects on established pulmonary arterial hypertension are modest, and no convincing evidence for in vivo inhibition of TGF-beta-driven target genes is presented | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
male sprague-dawley rats | - |
Source Tissue | Comment | Organism | Textmining |
---|
Synonyms | Comment | Organism |
---|---|---|
activin receptor-like kinase-5 | - |
Rattus norvegicus |
ALK-1 | - |
Rattus norvegicus |
BMPR-II | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000034 | - |
- |
Rattus norvegicus | 3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)benzamide |
Organism | Comment | Expression |
---|---|---|
Rattus norvegicus | exposure to monocrotaline and chronic hypoxia leads to a reduction in the expression of BMPR-II mRNA in rat lungs by day 21 | down |
General Information | Comment | Organism |
---|---|---|
malfunction | mutations in the TGF-type I receptor, activin receptor-like kinase (ALK)-1, cause hereditary hemorrhagic telangiectasia but have also been found in some cases of severe pulmonary arterial hypertension | Rattus norvegicus |