Integrin Inhibitor

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.

THR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis.

Furtisetabart is a humanized monoclonal antibody targeting CD147 with anti-tumor activity. Furtisetabart is of the human IgG4κ antibody subtype, and the recommended isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with K_d 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.

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4^DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC₅₀ of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML).

Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.

CWHM-12 is a potent inhibitor of αV integrins with IC₅₀s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.

Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.

Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models.

Nexinhib20 is an inhibitor that targets the interactions of Rab27a-JFC1 (IC₅₀: 2.6 μM) and Rac-1-GTP. Nexinhib20 can inhibit neutrophil exocytosis, adhesion, and β2 integrin activation, and has anti-inflammatory activity. Nexinhib20 can be used in the research of diseases such as systemic inflammation and myocardial ischemia-reperfusion injury.

TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .

Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity.

Caplacizumab (His Tag) is a humanized anti-von Willebrand factor (vWF) nanobody. Caplacizumab (His Tag) inhibits the binding of vWF with platelet glycoprotein (GP) Ibα. Caplacizumab (His Tag) inhibits the vWF-mediated platelet adhesion and prevents further microthrombi formation. Caplacizumab (His Tag) can be used for the research of thrombotic thrombocytopenic purpura (TTP).

Cilengitide is a potent and selective integrin inhibitor for α_vβ₃ and α_vβ₅ receptor, with IC₅₀ values of 4 nM and 79 nM, respectively.

GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.

Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4⁺ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses.

Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC₅₀=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs).

BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease.

A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC₅₀ of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.