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Catalog No.
Product Name
Application
Product Information
Citations
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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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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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α9β1/α4β1 integrin inhibitor
BOP sodium salt is a novel dual alpha9beta1/alpha4beta1 integrin inhibitor. -
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. -
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 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. -
αvβ3 Integrin Inhibitor
Cyclo(-RGDfK) TFA is a highly potent and selective inhibitor of the αvβ3 integrin, exhibiting an IC50 value of 0.94 nM. This cyclic peptide effectively targets tumor microvasculature and cancer cells by specifically binding to the αvβ3 integrin on the cell surface. It serves as a valuable tool in cancer research and therapeutic development, particularly in studies focused on angiogenesis and metastasis. -
Integrin Inhibitor
αvβ5 integrin-IN-1 is a selective inhibitor of the αvβ5 integrin, demonstrating a pIC50 of 8.2. This compound exhibits an impressive 800-fold selectivity for αvβ5 over αvβ3, making it a valuable tool in the study of integrin-mediated processes. Its primary applications include investigating cell adhesion, migration, and various pathways involved in cancer progression and tissue regeneration. -
Integrin Inhibitor
Gly-Arg-Gly-Asp-Ser (GRGDS) is a pentapeptide that acts as an integrin inhibitor by binding to integrin receptors αvβ3 and αvβ5. This binding disrupts cell adhesion processes, making it valuable in research applications related to cell migration, angiogenesis, and tumor progression. With estimated IC50 values of approximately 5 μM and 6.5 μM for its primary targets, GRGDS is a crucial tool for studies involving extracellular matrix interactions and integrin-mediated signaling pathways. -
αvβ3/αvβ5 integrin/IGF1R Inhibitor
Synstatin (92-119) is a potent inhibitor targeting αvβ3/αvβ5 integrins and IGF1R, exhibiting anti-angiogenic, anti-proliferative, antioxidant, and anti-tumor properties. It functions by competitively inhibiting the interaction of syndecan-1 with these integrins and IGF1R, thereby disrupting the ternary complex formation and blocking critical downstream signaling pathways. This compound is particularly relevant for research in cancer biology, especially in studies focused on angiogenesis and hepatocellular carcinoma. -
ανβ1 Integrin Inhibitor
PLN-1474 is a selective ανβ1 integrin inhibitor with an IC50 value of less than 50 nM. This compound demonstrates significant biological activity by reducing pSMAD3/SMAD3 levels, hepatic collagen gene expression, and hepatic OHP concentration in mouse models of liver fibrosis. PLN-1474 is valuable for research focused on the prevention and treatment of fibrotic and cirrhotic diseases. -
Integrin Signaling Inhibitor
Integrin signaling inhibitor, mP13, targets integrin signaling pathways, effectively inhibiting both inside-out and outside-in signaling mechanisms. This compound disrupts critical processes such as fibrinogen binding, platelet adhesion, and clot retraction. Due to its significant biological activity, mP13 is an essential reagent for studies in hemostasis, thrombosis, and cardiovascular research applications. -
Integrin αvβ3 Inhibitor
LXW7 is an integrin αvβ3 inhibitor that features a cyclic peptide structure incorporating Arg-Gly-Asp (RGD). It demonstrates a high binding affinity to the αvβ3 integrin with an IC50 value of 0.68 μM. LXW7 is known to enhance the phosphorylation of VEGFR-2 and activate ERK1/2, contributing to its anti-inflammatory properties. This compound can be utilized in research focusing on angiogenesis, cancer progression, and inflammatory processes. -
Integrin Inhibitor
Rondaptivon pegol is a pegylated aptamer that acts as an integrin inhibitor by specifically blocking the interaction between von Willebrand factor (VWF) and platelet glycoprotein GPIb. This inhibition plays a critical role in preventing arterial thrombosis, making Rondaptivon pegol a valuable tool in cardiovascular research and the study of thrombotic disorders. Its unique mechanism of action positions it as a potential therapeutic candidate for conditions associated with excessive platelet aggregation. -
α4β7 Integrin Inhibitor
Emvistegrast is a quinolone derivative that functions as a selective inhibitor of the α4β7 integrin. This compound demonstrates significant potential in modulating immune responses and is particularly relevant for research into inflammatory bowel disease and other conditions associated with α4β7 integrin activity. Its oral bioavailability allows for convenient administration in various preclinical studies, facilitating investigations into its therapeutic efficacy. -
Integrin Inhibitor
Integrin-IN-2 is a pan αv integrin inhibitor that demonstrates oral bioavailability. It effectively enhances the binding affinities for αvβ6, αvβ3, αvβ5, and αvβ8, with pIC50 values of 7.8, 8.4, 8.4, and 7.4, respectively. This compound is valuable for research applications focused on cancer metastasis and fibrosis, providing a tool for investigating integrin-mediated cellular processes. -
αVβ8 Integrin Inhibitor
αVβ8-IN-1 is an αVβ8 integrin inhibitor that targets integrin-mediated signaling pathways. This compound has demonstrated efficacy in inhibiting tumor growth in models such as EMT6, CT26, KPC, and TKCC-10. It serves as a valuable research tool for studies investigating idiopathic pulmonary fibrosis (IPF), non-specific interstitial pneumonia (NSIP), and various tumor types. -
Integrin Inhibitor
FITC-Ahx-Gly-Arg-Gly-Asp-Ser-Pro is a fluorescently labeled integrin inhibitor designed to inhibit the binding of tumor cells to endothelial cells lining blood vessels. This compound, based on the GRGDSP peptide sequence, effectively reduces tumor cell adherence and has potential applications in cancer research, particularly in studies focused on metastasis and angiogenesis. Its fluorescent properties facilitate visualization and tracking in cellular studies. -
αvβ6/αvβ1 Integrin Inhibitor
Bexotegrast hydrochloride is a selective dual inhibitor of the αvβ1 and αvβ6 integrins. By inhibiting these integrins, Bexotegrast hydrochloride effectively blocks the activation of TGF-β1, which is crucial in preventing the fibrotic growth in tissues associated with idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). This compound serves as a valuable tool for research into fibrosis-related pathologies and therapeutic interventions for fibrotic diseases. -
α4β7 Integrin Inhibitor
α4β7 Integrin-IN-1 is a highly effective inhibitor of the α4β7 integrin, specifically blocking its interaction with MadCAM-1 with an EC50 value of 0.05 nM. This compound is primarily utilized in research applications related to inflammatory bowel disease, providing insights into therapeutic strategies targeting integrin-mediated pathways. Its high potency makes it a valuable tool for studying cell adhesion processes and related inflammatory mechanisms. -
α5β1 Integrin Inhibitor
α5β1 integrin-IN-1 is a highly selective inhibitor of the α5β1 integrin, demonstrating a pIC50 of 9.4 and over 10,000-fold selectivity for α5β1 compared to αVβ3 (pIC50 = 5.5). This compound effectively reduces airway smooth muscle tension by disrupting cellular tethering mechanisms. With favorable inhalation pharmacokinetics in rodent models, α5β1 integrin-IN-1 is a valuable tool for researchers investigating asthma and related respiratory conditions. -
Integrin Inhibitor
ATL 1102 is a second-generation antisense oligonucleotide targeting the CD49d mRNA, acting as an integrin inhibitor. This compound demonstrates significant biological activity in modulating immune responses and has potential applications in treating autoimmune disorders and other inflammatory conditions. Researchers can utilize ATL 1102 to investigate the role of integrin signaling in various disease models. -
Integrin β(3) Inhibitor
mP6 (Myr-FEEERA-OH) is an integrin β3 inhibitor that specifically targets the interaction between Gα13 and integrin β3, preserving talin-dependent integrin function. This myristoylated peptide effectively blocks GTP usage in Rac1, Rap1, and Rab7, thereby inhibiting the infection process in CHO-A24 cells. mP6 is valuable for research applications involving integrin signaling and modulation of cell adhesion pathways. -
α2β1 integrin Inhibitor
BTT-3034 is a sulfonamide derivative that selectively inhibits the α2β1 integrin, targeting its role in cell adhesion. It demonstrates significant biological activity by inhibiting cell adhesion to rat tail collagen I with an EC50 of 160 nM and a maximal effect of 86%. Additionally, BTT-3034 effectively inhibits collagen binding in an α2 integrin variant that carries the conformationally activating E318W mutation, making it a valuable tool for research in cellular adhesion and integrin biology. -
αLβ2 Integrin Inhibitor
αLβ2 integrin-IN-1 is an inhibitor of the αLβ2 integrin, designed to obstruct αLβ2 integrin-mediated cell adhesion. This compound is valuable for investigating the role of αLβ2 integrin in various inflammatory conditions and can aid in exploring therapeutic interventions for diseases characterized by aberrant cell adhesion and migration. Its application can enhance understanding of the molecular mechanisms underlying inflammatory responses. -
Integrin Inhibitor
αvβ1 integrin-IN-2 is a highly effective inhibitor of integrins αvβ1 and α5β1, exhibiting IC50 values of 0.9 nM and 33 nM, respectively. This compound also demonstrates inhibitory activity against additional integrins, including IC50s of 380 nM for αvβ3, 280 nM for αvβ5, 230 nM for αvβ6, and 87 nM for αvβ8, as determined by the SPRA assay. αvβ1 integrin-IN-2 is valuable for research applications focused on integrin-mediated signaling pathways and cell adhesion processes. -
Integrin Inhibitor
Gly-Arg-Gly-Asp-Ser TFA is a pentapeptide that serves as an integrin inhibitor. It effectively binds to the integrin receptors αvβ3 and αvβ5, exhibiting an estimated IC50 of approximately 5 μM and 6.5 μM, respectively. This compound is valuable in research applications focused on cell adhesion, migration, and signaling processes relevant to various pathologies, including cancer and tissue engineering. -
αvβ6 Integrin Inhibitor
GSK3335103 is an orally active, non-peptide inhibitor of the αvβ6 integrin, demonstrating a potent affinity with a pIC50 value of 8. This compound is primarily utilized in research focused on pulmonary fibrosis, aiding in the understanding of its pathophysiology and potential therapeutic interventions. The inhibition of αvβ6 integrin by GSK3335103 can provide insights into cellular mechanisms involved in fibrotic processes. -
Integrin α4β1 Inhibitor
TBC3486 is a selective inhibitor of integrin α4β1. This compound enhances the sensitivity of leukemia cells to chemotherapy, demonstrating its potential as a chemosensitizer. TBC3486 shows efficacy in preclinical models related to integrin α4-dependent inflammatory and autoimmune conditions, notably in a mouse model of autoimmune encephalomyelitis. It is a valuable reagent for research focused on precursor B-cell acute lymphoblastic leukemia. -
α4 integrin Inhibitor
6-B345TTQ is an α4 integrin inhibitor that disrupts the interaction between α4 integrin and Leupaxin. This compound exhibits significant potential in the study of inflammatory processes and related pathways. Its inhibitory activity on α4 integrin places it at the forefront of research involving immune modulation and inflammation-related conditions. -
Integrin Receptors Inhibitor
Risuteganib is a synthetic RGD (arginyl-glycyl-aspartic acid)-class peptide functioning as an integrin receptor inhibitor. It effectively downregulates oxidative stress and restores homeostasis, targeting three integrin receptors associated with dry age-related macular degeneration (AMD). This compound is valuable for research applications focused on retinal health and the mechanisms underlying AMD. -
αvβ6 Integrin Inhibitor
αvβ6 integrin inhibitor 2 is a selective inhibitor of the αvβ6 integrin, demonstrating an IC50 of 96.5 nM. This compound effectively modulates integrin-mediated cell adhesion and signaling pathways, making it valuable for research in cancer metastasis, fibrosis, and tissue regeneration. Its ability to inhibit αvβ6 integrin activity positions it as a crucial tool for studying integrin-related biological processes.
