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Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated as crucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family, including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appear to promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, the functions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling, including the PI3K/Akt- and Ras/MAPK-dependent pathways.

Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulation of these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state. Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process via activation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.

Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one β subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit can form heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, and αv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be a common function of multiple αv integrins.

Cat. No.	Product Name	CAS No.	Information
H9617	ADH-503	2055362-72-4	ADH-503 is a small-molecule allosteric agonist of CD11b that can render tumors more sensitive to checkpoint blockade;ADH-503 rapidly decreased the genes involved in IL-1 signaling, increased the expression of cytokines involved in T cell and DC trafficking.ADH-503 reduced the regulatory T cell (Treg) recruitment of cytokines CCL17 and CCL22 in PDAC-activated macrophages, down-regulated TGF-β1, IL-1α, and IL-1β and reduced alternative activation markers arginase-1 (Arg1), YM1, and Retnlα while upregulating type I interferons (IFNα1 and IFNβ) and T cell recruitment factors (CXCL9, CXCL10, and CXCL11).DH-503 reduced the numbers of total tumor-infiltrating CD11b+cells and subsets of CD11b+ monocytes, granulocytes, eosinophils, and macrophages on myeloid cells, improves T cell responses in vivo, induces the accumulation of CD103+ cDCs in the tumor.ADH-503 impairs tumor growth and improves survival in orthotopic models and KPC GEMMs, also improves the efficacy of chemotherapy.
H9537	Bexotegrast	2376257-44-0	Bexotegrast is a potent inhibitor of ανβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
H9382	BMS587101	509083-77-6	BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research.
H9216	ATN-161	262438-43-7	ATN-161 (Ac-PHSCN-NH2) is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
H8559	THI0019	1378532-99-0	THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
H2354	α2β1 integrin-IN-15	916734-43-5	α2β1 integrin-IN-15 highly potent, selective, allosteric small-molecule inhibitor of integrin α2β1 with IC50 of 12 nM; ihibits adhesion of cells expressing wild-type (WT) and demonstrates no effect on RBL cells expressing an activating I-domain mutation (E318A), inhibits an activating cytoplasmic domain mutant [Del(GFFKR)] with an IC50 ≈4-fold higher than for wild-type integrin α2β1; shows efficacious activity in an animal model of arterial thrombosis.
H2353	Zaurategrast	455264-31-0	A potent and selective, orally bioavailable α4 integrin (α4β1/VLA-4 and, to a lesser extent, α4β7 integrin) antagonist, an ester prodrug of CT-7758; is developed for the treatment of multiple sclerosis.
H2352	Valategrast hydrochloride	828271-96-1	Valategrast hydrochloride is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.
H2351	Valategrast	220847-86-9	Valategrast is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.
H2350	TR-14035	232271-19-1	A potent, orally bioavailable, dual α4β7/α4β1 integrin antagonist with IC50 of 7/87 nM; blocks the binding of human α4β7 to an (125)I-MAdCAM-Ig fusion protein with IC50 of 0.75 nM; suppresses antigen-induced lung interleukin (IL)-5 mRNA upregulation, inhibits the leukocyte rolling flux, adhesion and emigration induced by IL4 in rats.

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