Integrin Inhibitor

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).

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).

C16Y acetate is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acetate acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .

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.

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.

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.

Natalizumab (Anti-CD49d) (AN100226; BG00002) Solution is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d), blocking 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 solution 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, thereby exerting anti-inflammatory and immunomodulatory activity. Natalizumab (Anti-CD49d) solution is used in the study of relapsing-remitting multiple sclerosis (RRMS) and is also applied in the research of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab (Anti-CD49d) can also prevent lymphocytes from entering the central nervous system, thus preventing acute demyelinating relapses.

Abciximab (C7E3), a chimeric mouse/human monoclonal antibody fragment, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.

ABH (hydrochloride) is an orally active arginase inhibitor (K_i = 8.5 nM). ABH hydrochloride promotes NO production and reduces the expression of inflammatory response-related molecules (ICAM-1, VCAM-1, MCP-1). ABH hydrochloride improves erectile function, reduces lung damage, promotes wound healing, reduces arterial blood pressure, and improves vascular fibrosis.

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC₅₀ of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.

SGN-B6A is an ADC, which targets integrin beta-6 (ITGB6) through human IgG1 monoclonal antibody Sigvotatug (HY-P990764), and exhibits cytotoxicity against multiple integrin beta-6-positive cancer cell through mitotic inhibitor MMAE (HY-15162).

OS-2966 is a humanized antibody expressed in CHO cells, targeting Integrin b1/ITGB1/CD29. OS-2966 carries a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 145.5 kDa. The isotype control for OS-2966 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC₅₀ of 0.63 nM. Antifibrotic effects.