Catalog No.
Product Name
Application
Product Information
Citations
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VCAM-1 antagonist
CDP323 is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 binding to ??4-integrins- Mustafa Ahmadzai, .et al. , Front Immunol, 2015, 6: 525 PMID: 26539194
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Integrin inhibitor
Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.- Yi Han Tan, .et al. , Cell Microbiol, 2017, Aug;19(8) PMID: 28186697
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Integrin inhibitor
Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.- Marion Bouvet, .et al. , Sci Rep, 2020, 10: 11404 PMID: 32647159
- Rosalie Richards, .et al. , bioRxiv, 2018, 15 Oct 2018
- Hiroki Kanazawa, .et al. , PLoS One, 2017, 12(2): e0173051 PMID: 28235037
- Yasuda J, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2017, Nov;390(11):1135-1144 PMID: 28785775
- Yasuda J, .et al. , Eur J Pharmacol, 2017, Jul 15;807:64-70 PMID: 28457922
- Hsian-Yu Wang, .et al. , Onco Targets Ther, 2016, 9: 2961-2973 PMID: 27284246
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α4β1/α4β7 integrin antagonist
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).- Higuchi S, .et al. , Dev Growth Differ, 2016, Sep;58(7):586-99 PMID: 27633818
- Pyrintegrin is a cell-permeable small molecule that promotes human embryonic stem cell (hESC) survival by > 30-fold.
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Integrin agonist
Leukadherin 1 is an allosteric activator of CD11b/CD18. Increases CD11b/CD18-dependent cell adhesion to fibrinogen (EC50 = 4 μM). -
αvβ3 integrin inhibitor
Cyclo (-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin.- Julian Tu, .et al. , Synlett, 2020, 31, A-F
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Inhibits integrin binding to RGD motifs
RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins.- Kan Zhang, .et al. , Exp Neurol, 2021, Feb 26;340:113659 PMID: 33640375
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Integrin inhibitor
Cyclo(RGDyK) trifluoroacetate is a potent and selective alphaVbeta3 integrin inhibitor with IC50 of 20 nM. -
αV integrins inhibitor
CWHM 12 can suppress all 5 alpha V integrins. CWHM12 not only worked the same way to prevent fibrosis as the genetic deletion method, it also prevent the progression of existing fibrosis in the liver and lungs and reversed some of the damage caused by fibrosis to those organs. -
α4β1/α9β1 inhibitor
R-BC154 is a high affinity fluorescent α4β1/α9β1 inhibitor. -
α1β1 inhibitor
Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.- Stephanie W Watts, .et al. , Pharmacol Res, 2024, Jun 14:206:107269 PMID: 38880313
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GpIIb/IIIa antagonist
GR 144053 trihydrochloride is a potent and selective platelet fibrinogen receptor glycoprotein IIb/IIIa (GpIIb/IIIa) antagonist. -
glycoprotein IIb/IIIa antagonist
Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation. -
α9β1/α4β1 integrin inhibitor
BOP sodium salt is a novel dual alpha9beta1/alpha4beta1 integrin inhibitor. -
LFA-1 Antagonist
BMS-688521 is a small molecule antagonist of leukocyte function associated antigen-1 (LFA-1). -
LFA-1 antagonist
Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. -
platelet glycoprotein IIb/IIIa antagonist
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. -
α5β1-integrin ligand
c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM. -
α4β1/α4β7 integrin antagonist
Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders. -
integrin αvβ3 antagonist
Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent. -
integrin α5β1 antagonist
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model. -
αVβ3 integrin inhibitor
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM. -
α4 integrin receptor inhibitor
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities. -
integrin-ligand interactions inhibitor
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. -
α5β1 Integrin Agonist
α5β1 integrin agonist-1 is a potent agonist of the α5β1 integrin, exhibiting an EC50 of 1.5 nM. This compound also inhibits α4β1 integrin activity with an IC50 of 2.99 μM, as demonstrated in Jurkat/VCAM-1 adhesion assays. α5β1 integrin agonist-1 induces concentration-dependent apoptosis and activates the caspase 3/7 pathway in α5β1 integrin-expressing K562 cancer cells. This reagent is suitable for investigations into cancer biology, particularly in studies focusing on integrin-mediated signaling pathways. -
α5β1 Integrin Antagonist
K34c is a potent and selective antagonist of the α5β1 integrin. By inhibiting this integrin, K34c effectively reduces chemotherapy-induced premature senescence and enhances apoptosis. This compound is particularly valuable for research in glioblastoma and provides insights into the modulation of tumor cell dynamics. -
α5β1 Integrin Antagonist
K34c hydrochloride is a selective antagonist of the α5β1 integrin, which plays a significant role in cell adhesion and migration. This compound effectively mitigates chemotherapy-induced premature senescence and enhances apoptosis in cellular models. K34c hydrochloride is particularly applicable in glioblastoma research, providing insights into tumor cell behavior and therapeutic responses. -
EDA-integrin Interactions Inhibitor
Irigenin is an inhibitor of EDA-integrin interactions, specifically targeting α9β1 and α4β1 integrins by blocking their binding sites on the C-C loop of Extra Domain A (EDA). This compound exhibits significant anti-cancer properties, particularly in gastric cancer cells, where it enhances TRAIL-induced apoptosis by increasing the expression of pro-apoptotic molecules. Irigenin may be valuable in cancer research, particularly in studies focused on metastasis and apoptosis modulation. -
Integrin ligand
VSLRGDTRG is a synthetic peptide derived from cadherin 17 (CDH17) that functions as a ligand for the α2β1 integrin. This peptide promotes the conformational activation of β1 integrin via the RGD motif, leading to enhanced cell adhesion and increased phosphorylation of FAK and ERK1/2. VSLRGDTRG is applicable in cancer research, specifically in studies involving tumors expressing CDH17, including colon and pancreatic cancers, where it may aid in understanding mechanisms of tumor proliferation and metastasis. -
Integrin αvβ6 Inhibitor
MORF-627 is a selective integrin αvβ6 inhibitor that effectively impairs TGF-β1 activation and pSMAD2 signaling. This compound significantly decreases collagen deposition and markers of epithelial-mesenchymal transition in fibrotic cells, demonstrating notable antifibrotic activity in idiopathic pulmonary fibrosis models without causing genotoxicity. While MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, these toxic effects can be mitigated by exogenous TGF-β. This reagent is valuable for investigating the pathological mechanisms underlying pulmonary fibrosis and assessing associated drug safety. -
αvβ6/αvβ1 Integrin Inhibitor
Bexotegrast is a potent oral dual inhibitor of the αvβ6 and αvβ1 integrins, with Kd values of 5.7 nM and 3.4 nM, respectively. This compound effectively inhibits TGF-β activation induced by αvβ6 and αvβ1, with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast demonstrates significant antifibrogenic properties and plays a critical role in blocking various pathways of TGF-β activation involved in fibrotic lung conditions. This makes it a valuable tool for research in fibrosis and related disorders. -
Integrin Inhibitor
GRGDSP is a synthetic linear RGD peptide that acts as an integrin inhibitor. It specifically interferes with integrin-mediated cell adhesion and signaling processes, making it a valuable tool in studies related to cell migration, angiogenesis, and tumor progression. GRGDSP can be utilized in various biological assays to explore integrin functions and their implications in disease models. -
α4β1 Integrin Agonist
Integrin Modulator 1 is a selective agonist for the α4β1 integrin, exhibiting an IC50 of 9.8 nM for RGD-binding activity. This compound promotes enhanced cell adhesion through α4β1 integrin with an EC50 of 12.9 nM. Its biological activity makes it valuable for research applications focused on cell adhesion processes and integrin-related signaling pathways. -
α4 Integrin Antagonist
Carotegrast methyl is a selective antagonist of the α4 integrin, acting to inhibit its interactions. This compound, along with its active metabolite HCA2969, functions as a dual antagonist of both α4β1 and α4β7 integrins. Carotegrast methyl has demonstrated efficacy in preventing the development of colitis in murine models, making it a valuable tool for research in inflammatory diseases and integrin-related pathways. -
Integrin Antagonist
Lifitegrast sodium is a potent integrin antagonist that disrupts the interaction between intercellular adhesion molecule 1 (ICAM-1) and lymphocyte function-associated antigen 1 (LFA-1). By blocking this binding, Lifitegrast sodium interrupts the T cell-mediated inflammatory response. It demonstrates significant inhibitory action on Jurkat T cell attachment to ICAM-1, with an IC50 of 2.98 nM. This reagent is primarily utilized in research related to dry eye disease and other inflammatory conditions.
