Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Integrin Antagonist
Tetrac (Tetraiodothyroacetic acid) acts as an integrin antagonist by selectively inhibiting the interaction of thyroid hormones, L-thyroxine (T4) and 3,5,3'-triiodo-L-thyronine (T3), with integrin αvβ3 receptors. This blockade disrupts downstream signaling pathways, leading to significant anti-angiogenic and anti-tumor effects. Tetrac is valuable for research in cancer biology and therapeutic approaches targeting tumor vascularization. -
αv-integrin Ligand
RGD-4C is a peptide characterized by the arginine-glycine-aspartic acid (ACDCRGDCFC) sequence, which specifically targets αv-integrins. This peptide's RGD motif mimics the binding sites of extracellular matrix proteins, facilitating interactions with integrins. RGD-4C serves as a valuable tool in research focused on cell adhesion, migration, and signaling, particularly in antitumor studies where it can be conjugated with bioactive molecules to enhance therapeutic efficacy in animal models. -
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. -
α5β1 Integrin Agonist
LT25 is an agonist of the α5β1 integrin, exhibiting an EC50 value of 9.9 nM. This compound promotes cell adhesion and migration through the activation of α5β1 integrin, making it valuable for research applications related to cancer metastasis, tissue engineering, and regenerative medicine. Its ability to modulate integrin activity makes LT25 an essential tool for studying cell-extracellular matrix interactions. -
αvβ3/αvβ5 Integrins Antagonist
SB-267268 is a selective antagonist of αvβ3 and αvβ5 integrins, demonstrating inhibition constants (Kis) of 0.9 nM, 0.5 nM, and 0.7 nM for human αvβ3, monkey αvβ3, and human αvβ5, respectively. This compound effectively inhibits angiogenesis, showcasing IC50 values of 0.68 nM for human αvβ3 and 0.29 nM for mouse αvβ3. SB-267268 is a valuable tool for research focused on vascular biology, cancer therapeutics, and the modulation of integrin signaling pathways. -
Integrin Antagonist
Surfactin C1 is an integrin antagonist known for its amphiphilic biosurfactant properties. It effectively inhibits the adhesion of leukemic HL-60 cells to human umbilical vein endothelial cells (HUVEC), demonstrating its capability to modulate cell adhesion dynamics. Additionally, Surfactin C1 impacts the expression of adhesion molecules, including ICAM-1 and VCAM-1, making it a valuable compound for research in cancer biology and vascular inflammation studies. -
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. -
α4β1/α4β7 Integrin Antagonist
RO0270608 is a dual α4β1/α4β7 integrin antagonist that functions by inhibiting integrin-mediated cell adhesion and migration. This compound exhibits significant anti-inflammatory activity and is primarily used in research focused on inflammatory diseases and immune response modulation. Its dual targeting makes it a valuable tool for investigating pathways related to vascular and mucosal adhesion in various biomedical applications. -
Integrin Ligand
Alkyne-cRGD is an integrin ligand that facilitates targeted binding to integrin proteins. This compound is valuable in the study of protein degraders and can be utilized in copper-catalyzed azide-alkyne cycloaddition reactions for bioconjugation applications. Its ability to selectively interact with integrins makes it a key tool in cancer research and various therapeutic studies. -
α7β1 Integrin Modulator
α7β1 integrin modulator-1 is a potent modulator of the α7β1 integrin, a crucial receptor involved in cell adhesion and signaling. This compound shows promise in enhancing muscle regeneration and function, making it a valuable tool for research into muscular dystrophy and related muscle-wasting diseases. Its modulatory effects on integrin activity may elucidate mechanisms underlying muscular disorders and aid in the development of therapeutic strategies. -
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. -
Integrin Control
RGD Negative Control is a selective integrin control used in biological assays. This compound serves as a non-active counterpart to RGD, allowing researchers to accurately assess the specificity and activity of RGD-targeted therapies. It is particularly useful for studies involving cell adhesion, migration, and the interaction of integrins with extracellular matrix components in various biological contexts. -
α4β7 Integrin Antagonist
α4β7 Integrin-IN-2 is a potent antagonist of human α4β7 integrin, demonstrating an IC50 of less than 5 nM. This compound effectively modulates α4β7 integrin-mediated biological pathways, making it a valuable tool for investigating inflammatory diseases. Its strong inhibitory activity positions it for use in research aimed at understanding mechanisms of inflammation and potential therapeutic interventions. -
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. -
α4 Integrin Antagonist
GW559090 is a selective α4 integrin antagonist that competitively inhibits α4β1 with a Kd of 0.19 nM. It effectively disrupts the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin, with IC50 values of 7.72 nM and 8.04 nM, respectively. Additionally, GW559090 inhibits the α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) interaction (IC50 = 23 nM). This compound has potential applications in research focused on inflammatory conditions such as Sjögren's syndrome and related dry eye disorders. -
α4 Integrin Receptor Antagonist
α4 integrin receptor antagonist 3 is a potent orally active antagonist of the α4 integrin receptor. It effectively inhibits the adhesion of K562 cells through the α4β1/VCAM-1 and α4β7/MAdCAM-1 interactions, demonstrating IC50 values of 130 nM and 2 nM, respectively. This compound is suitable for research applications involving inflammatory disorders and may be particularly useful in the study of dextran sulfate sodium (DSS) colitis models. -
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. -
α4β1 Integrin Antagonist
CP-664511 is a potent α4β1 integrin antagonist with an IC50 of 0.52 nM, exhibiting significant anti-inflammatory properties. By inhibiting the interaction between α4β1 integrin and vascular cell adhesion molecule-1 (VCAM-1), CP-664511 effectively reduces eosinophil infiltration into lung tissue. This compound is valuable for investigating mechanisms underlying asthma and allergic airway diseases. -
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 Anagonist
Ac-RGDS-NH2 is a tetrapeptide that serves as an integrin antagonist. It exhibits competitive binding to the GPIIb/IIIa receptor with a Ki of 4.2 μM, effectively inhibiting the interaction of fibrinogen with platelets and consequently suppressing platelet aggregation. This reagent is suitable for research applications related to thrombosis and platelet function studies. -
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 Antagonist
UR-2922 is an integrin antagonist that selectively targets the GPIIb/IIIa receptor on platelets. This compound exhibits potent antiplatelet aggregation activity, making it a useful tool for research into cardiovascular diseases. With its high affinity for human platelet receptors and favorable pharmacokinetic properties, UR-2922 is ideal for studies aimed at understanding and inhibiting cardiovascular pathophysiology. -
alpha V Integrin Antagonist
JNJ-26076713 is a potent and orally active antagonist of alpha V integrins, showing IC50 values of 2.3 nM for alpha(V)beta(3) and 6.3 nM for alpha(V)beta(5). This compound effectively inhibits retinal neovascularization, making it a valuable tool for research in vascular biology and potential therapeutic applications in ocular diseases. Its specificity for alpha V integrins positions JNJ-26076713 as a significant reagent for studying integrin-mediated 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 αvβ3 Ligand
c-RGD-SH is a selective ligand for integrin αvβ3, playing a crucial role in tumor cell adhesion and migration. When conjugated with core-crosslinked polymeric micelles (CCPM), it can be utilized to synthesize a dual modality nanoparticle probe. This probe, labeled with Cy7 and 111In, facilitates both SPECT and near-infrared fluorescence (NIRF) imaging in tumor research applications, enabling enhanced visualization and targeting of cancerous tissues. -
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. -
Integrin
Arg-Gly-Asp TFA is a synthetic peptide that targets integrins, specifically interacting with αVβ1, αVβ3, αVβ5, αVβ6, αVβ8, α8β1, and α5β1. This peptide is crucial for mediating cell adhesion and serves as a fundamental component in the design of radioligands and peptidomimetics. Applications include the study of integrin expression and activity in vivo, providing insights into cellular interactions and behaviors relevant to various biological processes. -
Integrin Anatgonist
L-739758 is an antagonist of the αIIbβ3 integrin, also known as platelet glycoprotein IIb/IIIa. This peptidomimetic compound mimics the RGD (arginine-glycine-aspartic acid) motif, effectively binding to αIIbβ3 integrin and interfering with the blood coagulation process. L-739758 inhibits platelet aggregation, making it valuable for research focused on thrombosis and related cardiovascular disorders. -
α4 Integrin Antagonist
Carotegrast methyl hydrochloride is a potent and selective antagonist of the α4 integrin. It demonstrates significant biological activity by inhibiting the interactions mediated by α4β1 and α4β7 integrins, effectively preventing the development of colitis in murine models. This compound is valuable for research applications in understanding inflammatory processes and exploring therapeutic strategies in autoimmune diseases. -
GPIIb/IIIa Integrin
Gantofiban is a potent antagonist of the GPIIb/IIIa integrin receptor. Its mechanism involves binding to this receptor, which leads to the inhibition of platelet aggregation, producing a significant antithrombotic effect. Gantofiban is primarily used in research related to thrombosis, cardiovascular diseases, and the study of platelet function. -
Integrin α5β1 Inhibitor
CLT-28643 is an integrin α5β1 inhibitor that plays a significant role in modulating cellular adhesion and migration. It effectively reduces the overexpression of integrin α5β1 in post-surgical blebs, thereby facilitating the wound healing process. This compound is valuable for research in tissue regeneration and healing mechanisms. -
Integrin Inhibitor
RUC-1 is a specific inhibitor of the αIIbβ3 integrin. This compound effectively inhibits fibrin deposition and platelet aggregation in mouse models expressing hybrid hαIIb/mβ3 receptors. RUC-1 demonstrates significant antithrombotic effects, making it a valuable tool for studying integrin-related processes and potential therapeutic applications in coagulation disorders. -
Integrin Antagonist
Zaurategrast ethyl ester sulfate serves as an antagonist for the α4β1 and α4β7 integrins. This compound demonstrates significant efficacy in modulating immune responses, making it a valuable tool for investigating therapeutic strategies in inflammatory and autoimmune disorders. Its mechanism of action supports research focused on the modulation of integrin-mediated cell adhesion and migration.
