Integrin Inhibitor

Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) is an anti-mouse/human VLA-4/CD49d IgG2b monoclonal antibody. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can reduce VLA-4 positive cells. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can inhibit the migration of Tc1 cells to tumors. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) inhibits the retention of leukemia cells in the spleen and bone marrow by blocking VLA-4. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can be used for research on inflammation conditions and cancer such as experimental autoimmune encephalomyelitis (EAE), melanoma and leukemia.

Risuteganib hydrochloride is a synthetic RGD (arginyl-glycyl-aspartic acid)-class peptide. Risuteganib hydrochloride is an anti-integrin that downregulates oxidative stress and restores homeostasis, and targets three integrin receptors that are implicated in dry age-related macular degeneration (AMD) in order to restore homeostasis in the retina.

G-Pen-GRGDSPCA TFA is an αvβ3-inhibiting RGD peptide. G-Pen-GRGDSPCA can limit neointimal hyperplasia and lumen stenosis after vascular injury, as well as regulate the migration and proliferation of smooth muscle cells. G-Pen-GRGDSPCA TFA can be used in the study of the mechanism of vascular injury repair.

LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.

Isoastragaloside I is a natural compound found in Astragalus membranaceus, with oral activity and multiple biological activities such as anti-inflammatory and antioxidant properties. Isoastragaloside I inhibits Akt, NF-κB, MAPKs and PI3K, enhances the activity of hepatic FXR, regulates the TGF-β/Smads signaling pathway, and upregulates antioxidant molecules downstream of Nrf2. Isoastragaloside I inhibits the expression of NO, TNF-α, iNOS, COX-2, IL-1β and VCAM-1, and reduces intracellular ROS levels. Isoastragaloside I attenuates blood-brain barrier disruption, restores intestinal barrier function, increases β-cell mass, improves glucose homeostasis, and elevates circulating adiponectin levels. Isoastragaloside I can be used for the study of neuroinflammation-related neurodegenerative diseases, cholestatic liver disease, and diabetes.

RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD⁺ site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC₅₀=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections.

Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC₅₀ values of 7.8, 8.4, 8.4 and 7.4, respectively.

Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research .

Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA, a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used in the research of tumors.

Rondaptivon pegol (BT200) is a pegylated aptamer targeting von Willebrand factor (VWF), with an EC₅₀ of 33 nM in humans. Rondaptivon pegol effectively alleviates acute myocardial ischemia-reperfusion injury in mice by inhibiting VWF activity, reducing microvascular obstruction, inflammatory responses and cardiomyocyte apoptosis (apoptosis). Rondaptivon pegol inhibits the binding of VWF to platelet glycoprotein GPIb, thereby preventing arterial thrombosis in cynomolgus monkeys. Rondaptivon pegol can be used in research related to arterial thrombosis, stroke, myocardial infarction and myocardial ischemia-reperfusion injury.

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.

Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke.

αVβ8-IN-1 is a αVβ8 integrin inhibitor. αVβ8-IN-1 has been shown to inhibit the growth of tumors such as EMT6, CT26, KPC, and TKCC-10. αVβ8-IN-1 can be used in research related to idiopathic pulmonary fibrosis (IPF), non-specific interstitial pneumonia (NSIP), and tumors.

FITC-Ahx Gly Arg Gly Asp Ser Pro is a GRGDSP (HY-P0290) coupled to FITC. GRGDSP is an integrin inhibitor that can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis.

ITGB3-IN-1 is an orally active integrin subunit beta 3 ITGB3 inhibitor with a K_d of 7.26 μM. ITGB3-IN-1 exhibits potent anti-orthopoxvirus effects with an EC₅₀ for vaccinia virus (VACV) of 1.82 μM. ITGB3-IN-1 inhibits hERG with an IC₅₀ of 1.13 μM. ITGB3-IN-1 can be used for the study of orthopoxvirus.

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

mP6 (Myr-FEEERA-OH) TFA is a myristoylated peptide. mP6 TFA inhibits the interaction of Gα13 with integrin β3 without disrupting talin-dependent integrin function. mP6 TFA can block the GTP usage of Rac1, Rap1, and Rab7, effectively inhibiting the infection of CHO-A24 cells.

Anti-LFA-1α/CD11a Antibody (TS-1/22.1.1.13) is a kind of mouse IgG1 chimeric antibody inhibitor, targeting to human LFA-1α/CD11a. Anti-LFA-1α/CD11a Antibody (TS-1/22.1.1.13) reacts with human LFA-1α (lymphocyte function-associated antigen 1 alpha) also known as integrin alpha L chain and CD11a. Anti-LFA-1α/CD11a Antibody (TS-1/22.1.1.13) can be used for the researches of immunology and infection, such as human immunodeficiency virus (HIV).

Erlizumab (rhuMAb) is a monoclonal antibody against the Integrin b2/ITGB2/CD18 subunit of the Mac-1 receptor. Erlizumab can reduce reperfusion injury in myocardial infarction.

RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC₅₀ of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.