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GSK3008348 is an integrin alphaVbeta6 inhibitor (Ki = 0.01 nM). It is selective for integrin alphaVbeta6 over integrins alphaVbeta1, alphaVbeta3, alphaVbeta5, and alphaVbeta8 (IC50s = 3.9, 50, 1,000, 126, and 16 nM, respectively, in cell adhesion assays). GSK3008348 induces internalization and degradation of integrin alphaVbeta6 and reduces the phosphorylation of SMAD2 in normal human bronchial epithelial (NHBE) cells. Intranasal administration of GSK3008348 (3 mg/kg) decreases lung collagen levels in a mouse model of lung fibrosis induced by bleomycin (Cay13877). SMILES OC(C[C@@H](C1=CC(N2N=C(C)C=C2C)=CC=C1)CN3C[C@H](CCC(N4)=CC=C5C4=NCCC5)CC3)=O InChi Code InChI=1S/C29H37N5O2/c1-20-15-21(2)34(32-20)27-7-3-5-24(16-27)25(17-28(35)36)19-33-14-12-22(18-33)8-10-26-11-9-23-6-4-13-30-29(23)31-26/h3,5,7,9,11,15-16,22,25H,4,6,8,10,12-14,17-19H2,1-2H3,(H,30,31)(H,35,36)/t22-,25-/m1/s1 InChi Key ZMXBIIQMSGOIRZ-RCZVLFRGSA-N
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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