Name | FAPL-PI3Ki1 |
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Description | FAPL-PI3Ki1 is a specific FAP-targeted PI3K inhibitor that selectively targets FAP-expressing human IPF lung fibroblasts and potently inhibits collagen synthesis.FAPL-PI3Ki1 significantly inhibited phosphorylation of Akt in IPF fibroblasts with IC50 of 200 nM, also inhibited phosphorylation of 4E-BP1.FAPL-PI3Ki1 induced suppression of TGFb1-stimulated collagen production and phosphorylation of Akt in IPF fibroblasts requires participation of FAP.FAPL-PI3Ki1 suppressed production of hydroxyproline (major building block of collagen), reduced collagen deposition, and increased mouse survival in a mouse model of IPF inhibited PI3K activation in fibrotic lungs. |
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References | 1. Suraj U Hettiarachchi, et al. Sci Transl Med. 2020 Oct 28;12(567):eaay3724. |
Molecular Formula | C52H48F4N10O12S3 |
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Molecular Weight | 1177.188 |