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Chemical Structure : GSK3335103
Catalog No.: PC-72274Not For Human Use, Lab Use Only.
GSK3335103 (GSK-3335103) is a potent, oral, small molecule RGD-mimetic αvβ6 integrin inhibitor with pKi of 9.96.
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GSK3335103 (GSK-3335103) is a potent, oral, small molecule RGD-mimetic αvβ6 integrin inhibitor with pKi of 9.96.
GSK3335103 was shown to have a minimum of 4-fold (αvβ3) and a maximum >91,201 (αIIbβ3) selectivity over the other RGD integrins.
GSK3335103 caused a concentration-dependent internalisation of αvβ6 in NHBE cells with a pEC50 of 9.35.
Treatment with GSK3335103 resulted in a concentration-dependent reduction in pSmad2 signalling in NHBE cells with a pIC50 value of 8.19, also inhibited pSmad2 signalling in a concentration-dependent manner with a comparable potency in an ex vivo IPF PCLS system.
GSK3335103 inhibit the activation of TGFβ in a murine model of bleomycin-induced lung fibrosis, as measured by αvβ6 engagement, TGFβ signalling and collagen deposition, with a prolonged duration of action observed in vivo.
| M.Wt | 485.6 | |
| Formula | C27H36FN3O4 | |
| Appearance | Solid | |
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1. Alex L Wilkinson, et al. Eur J Pharmacol. 2021 Dec 15;913:174618.
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