XRF-1021 is an orally active inhibitor of Homer-interacting protein kinase 2 (HIPK2), with an IC50 value of 0.18 μM. It effectively decreases the expression of fibrotic markers such as Fibronectin, Collagen I, and α-SMA in TGF-β1 stimulated renal cell lines, including NRK-49F and HK-2. XRF-1021 further inhibits key signaling pathways including TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch. This compound demonstrates potential in reducing renal injury and fibrosis in vivo, making it a valuable tool for research on chronic kidney disease.
XRF-1021 is an orally active inhibitor of Homer-interacting protein kinase 2 (HIPK2), with an IC50 value of 0.18 μM. It effectively decreases the expression of fibrotic markers such as Fibronectin, Collagen I, and α-SMA in TGF-β1 stimulated renal cell lines, including NRK-49F and HK-2. XRF-1021 further inhibits key signaling pathways including TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch. This compound demonstrates potential in reducing renal injury and fibrosis in vivo, making it a valuable tool for research on chronic kidney disease.
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