1893340-21-0
Chemical Structure
GSK3335103
- CAS No.: 1893340-21-0
- Formula:C27H36FN3O4
- Molecular Weight:485.59
InChIKey: MKIJZIVRJUMEAD-AMGIVPHBSA-N
SMILES: O=C(O)C[C@@H](C1=CC=CC(OCCOC)=C1)CN2C[C@@](CCC3=NC4=C(CCCN4)C=C3)(F)CC2
Biological Activity: GSK3335103 is an orally active non-peptidic αvβ6 integrin inhibitor with a pIC50 of 8 and a pKi of 9.96. GSK3335103 blocks αvβ6 integrin-mediated cell adhesion and TGF-β1 activation, induces integrin internalization, recycling and lysosomal degradation, attenuates TGFβ signaling and reduces collagen deposition. GSK3335103 decreases the level of pSmad2 in BAL cells and collagen deposition in lung tissues in a mouse model of pulmonary fibrosis. GSK3335103 can be used in research related to pulmonary fibrosis[1][2][3].
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GSK3335103 | GSK3335103 is an orally active non-peptidic αvβ6 integrin inhibitor with a pIC50 of 8 and a pKi of 9.96. GSK3335103 blocks αvβ6 integrin-mediated cell adhesion and TGF-β1 activation, induces integrin internalization, recycling and lysosomal degradation, attenuates TGFβ signaling and reduces collagen deposition. GSK3335103 decreases the level of pSmad2 in BAL cells and collagen deposition in lung tissues in a mouse model of pulmonary fibrosis. GSK3335103 can be used in research related to pulmonary fibrosis. | |||||||||||||||||||||
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References
- [1]. Procopiou PA, et al. Discovery and Development of Highly Potent and Orally Bioavailable Nonpeptidic αβ Integrin Inhibitors. Journal of medicinal chemistry. 2024 Oct 10;67(19):17497-17519. [Content Brief]
- [2]. Hryczanek HF, et al. Core Modifications of GSK3335103 toward Orally Bioavailable αβ Inhibitors with Improved Synthetic Tractability. Journal of medicinal chemistry. 2024 Nov 14;67(21):19689-19715. [Content Brief]
- [3]. Wilkinson AL, et al. Pharmacological characterisation of GSK3335103, an oral αvβ6 integrin small molecule RGD-mimetic inhibitor for the treatment of fibrotic disease. European journal of pharmacology. 2021 Dec 15;913:174618.
