αvβ5 Antagonist

Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC₅₀s of 0.61 nM (α_νβ₃), 8.4 nM (α_νβ₅) and 14.9 nM (α₅β₁), respectively. Cilengitide inhibits the binding of α_νβ₃ and α_νβ₅ to Vitronectin with IC₅₀s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.

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.

SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with K_i values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .

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.

SU015 (DOTA-RGDfK dimer) is a Integrin α_vβ₅ and α_vβ₃ antagonist. SU015 exhibits comparable affinity for α_vβ₅ and α_vβ₃, with relatively higher potency and specificity compared to other integrins. SU015 inhibits α_vβ₃-mediated cell adhesion to fibrinogen, α_vβ₃-mediated adhesion of activated platelets to osteopontin, and α_vβ₅-mediated cell adhesion to vitronectin. SU015 shows potent inhibitory effects on FGF2-induced angiogenesis in the CAM model. SU015 carries a linker arm available for radioisotope conjugation, and acts as a target-specific radioreagent when labeled with ⁹⁰Y (i.e., RP697) or ¹⁷⁷Lu (i.e., RP688). SU015 can be used in studies related to tumor metastasis and tumors.

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.

JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC₅₀ values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization.