2. Signaling Pathways
  3. Cytoskeleton
  4. Integrin
  5. αvβ1 Isoform

αvβ1

The integrin αvβ1 is a heterodimeric transmembrane receptor that mediates cell adhesion and extracellular matrix interactions, playing a critical role in tissue remodeling and fibrotic processes[1][2][3]. Mechanistically, αvβ1 directly binds the latency-associated peptide of transforming growth factor-β1 (TGFβ1), facilitating TGFβ1 activation and promoting fibroblast differentiation in fibrotic tissues[1][2]. In disease models, selective αvβ1 inhibition attenuates bleomycin-induced pulmonary fibrosis and carbon tetrachloride-induced liver fibrosis, demonstrating its therapeutic potential in fibrosis-associated pathologies[1][3]. Compared with related isoforms such as αvβ3 and αvβ6, αvβ1 exhibits distinct ligand specificity and higher expression on activated fibroblasts, highlighting its unique functional profile[4][1][2]. Structurally optimized small-molecule inhibitors, including azabenzimidazolone derivatives, achieve potent αvβ1 selectivity without substantially affecting other integrins, providing precise tools for experimental modulation of TGFβ1-mediated fibrotic signaling[3]. Dual antagonists targeting αvβ1 and related integrins like α5β1 further enable the dissection of overlapping integrin pathways and the evaluation of combinatorial therapeutic strategies in airway hyperresponsiveness and fibrotic disease models[5]. Collectively, these studies establish αvβ1 as a critical regulator of fibrotic signaling, distinguishable from other RGD-binding integrins, and underscore the utility of selective inhibitors in preclinical research and potential clinical translation[1][2][3][5].

αvβ1 Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-137561
    Bexotegrast
    		Inhibitor 99.74%
    Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.
  • HY-15102
    MK-0429
    		Antagonist 99.50%
    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
  • HY-19767
    GSK 3008348
    		Antagonist 98.04%
    GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.
  • HY-19767A
    GSK 3008348 hydrochloride
    		Antagonist 99.86%
    GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.
  • HY-172494
    DSPE-PEG2000-iRGD
    DSPE-PEG2000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG2000-iRGD can be used for agent delivery.
  • HY-P10704
    C16Y
    		Inhibitor
    C16Y is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .