1-(2-Pyridin-2-yl-6,7dihydro-5H-cyclopenta[e]pyrimidin-4-yl)pyrrolo[3,2-c]pyridine, 2-(2-Pyridinyl)-4-(1H-pyrrolo[3,2-c]pyridin-1-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine, AZ 12601011, AZ-12601011
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AZ12601011 is an orally active, subtype-selective TGF-β type I receptors active site inhibitor (active-site affinity: ALK4/5/6 Kd = 2.6/2.9/42 nM, ALK1/2/3 Kd = 40/15/40 μM) that prevents ALK4/5/7-mediated Smad2, but not ALK1/2/3/6-mediated Smad1, phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12601011 inhibits 4T1 murine mammary carcinoma growth in cultures (IC50 = 400 nM) and in vivo (50 mg/kg bid. po. mice). AZ12601011 also causes heart valve lesions and physeal dysplasia in rats (150 mg/kg/day po. for 7 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
Orally active, subtype-selective TGF-β type I receptors ALK4/5/7 active site inhibitor in vitro and in vivo.
Liver injury results in rapid regeneration through hepatocyte proliferation and hypertrophy. However, after acute severe injury, such as acetaminophen poisoning, effective regeneration may fail. We investigated how senescence may underlie this regenerative failure. In human acute liver disease, and murine
Aberrant signaling by transforming growth factor-β (TGF-β) and its type I (ALK5) receptor has been implicated in a number of human diseases and this pathway is considered a potential target for therapeutic intervention. Transforming growth factor-β signaling via ALK5 plays
The metastatic process of colorectal cancer (CRC) is not fully understood and effective therapies are lacking. We show that activation of NOTCH1 signaling in the murine intestinal epithelium leads to highly penetrant metastasis (100% metastasis; with >80% liver metastases) in
The transforming growth factor β (TGFβ) superfamily includes TGFβ, activins, inhibins, and bone morphogenetic proteins (BMPs). These extracellular ligands have essential roles in normal tissue homeostasis by coordinately regulating cell proliferation, differentiation, and migration. Aberrant signaling of superfamily members, however
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