Pinatuzumab is a CD22 monoclonal antibody. Pinatuzumab targets the cell-surface antigen CD22. Pinatuzumab can be used for synthesis of antibody drug conjugates (ADCs) to research several diseases including non-Hodgkin lymphoma (NHL)[1][2].
SF0166 is a topically administered αvβ3 integrin antagonist, inhibits integrin-ligand interactions with IC50 of 0.6 nM to 13 nM for human αvβ3, αvβ6, and αvβ8; inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 of 7.6 pM-76 nM; significantly decreases neovascularization in the oxygen-induced retinopathy mouse models. Other Indication Phase 2 Clinical
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4].
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD)[1].
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
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[1] [2] .
Veltuzumab (IMMU-106) is a humanized anti-CD20 monoclonal antibody. Veltuzumab has low EC50 value of 0.08-0.09 μg/mL in the Daudi cell line. Veltuzumab can be used for the research of cancer including non-Hodgkin lymphoma (NHL)[1].
GR 144053 trihydrochloride is a selective and non-peptic GPIIb/IIIa inhibitor (IC50=37 nM)[1].
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[1].
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM; displays >1,000 fold selectivity against the most closely related b2-integrin Mac-1 and b1-integrin function; inhibits the production of IL-2 in human PBMC and whole blood with IC50 value of 3 nM and 120 nM, respectively; exhibits an attractive DMPK profile, BI-1950 is a excellent molecule for testing pharmacological hypotheses in vitro and in vivo.
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[1].
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)[1][2].
GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM; the rate of BIO7662 binding is dependent on the metal ion concentration; directly competes with VCAM-1, CS-1, and BIO1211 for binding to the integrin.
Cyclo(Arg-Gly-Asp-D-Phe-Val) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia[1].
BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders[1].
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity[1][2].
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) (extracted from patent WO2020210404A1, compound 5)[1].
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].
Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer[1].
A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively[1][2].
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
αvβ6 integrin inhibitor 2 is a potent ανβ6 integrin inhibitor with an IC50 of 96.5 nM (WO2020081154A1, example 19)[1].
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].
EILEVPST is a recombinant human fibronectinderived low-molecular-weight peptide fragment. EILEVPST can promote cell type-specific α4 integrin-mediated adhesion. EILEVPST can be used for the research of thrombogenesis[1].
Tirofiban (L700462) hydrochloride is a Gp IIb/IIIa receptor antagonist of nonpeptide derivative of tyrosine. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2].