Catalog No.
Product Name
Application
Product Information
Citations
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PAK1 Inhibitor
AZ13705339 is a potent and selective PAK1 inhibitor that exerts its action with IC50 values of 0.33 nM for PAK1 and 59 nM for phosphorylated PAK1 (pPAK1). This compound displays strong binding affinities for PAK1 and PAK2, with dissociation constants (Kd) of 0.28 nM and 0.32 nM, respectively. AZ13705339 is primarily utilized in cancer research, providing insights into PAK1-mediated signaling pathways. -
PAK Inhibitor
G-5555 hydrochloride is a selective inhibitor of p21-activated kinase 1 (PAK1), exhibiting a potency with a Ki value of 3.7 nM. This compound is useful in research focused on cell signaling pathways and oncogenesis, particularly in studies exploring the role of PAK1 in cancer progression and metastasis. G-5555 hydrochloride can be used to elucidate the biological functions of PAK1, aiding in the development of targeted therapeutic strategies. -
PAK1 Inhibitor Probe
NVS-PAK1-C is a specific allosteric inhibitor of the PAK1 protein, exhibiting ATP-competitive activity with IC50 values of 5 nM and 6 nM for dephosphorylated and phosphorylated PAK1, respectively. Additionally, NVS-PAK1-C demonstrates inhibitory effects on PAK2, with IC50 values of 270 nM for dephosphorylated PAK2 and 720 nM for phosphorylated PAK2. This compound serves as a valuable tool for research applications focused on elucidating the role of PAK1 and PAK2 in various cellular processes and signaling pathways. -
PAK1 Inhibitor
PAK1-IN-1 is a selective inhibitor of PAK1, exhibiting an IC50 of 9.8 nM. This compound effectively inhibits the migration and invasion of tumor cells associated with PAK1 activity in a dose-dependent fashion. PAK1-IN-1 serves as a valuable tool for research related to cancer biology and the exploration of therapeutic strategies targeting PAK1 signaling pathways. -
PAK Inhibitor
G-9791 is a potent inhibitor of p21-activated kinases (PAK) with high affinity characterized by Ki values of 0.95 nM for PAK1 and 2.0 nM for PAK2. This pyridone side chain analogue demonstrates significant biological activity, making it a valuable tool for studying the PAK signaling pathway. G-9791 is widely applicable in cancer research and investigations into cellular processes regulated by PAK kinases. -
PAK1 Inhibitor
2,2′-Dihydroxy-6,6′-dinaphthyl disulfide is a selective PAK1 inhibitor, targeting the p21-activated kinase 1 protein with notable specificity. This compound has demonstrated the ability to modulate cellular signaling pathways linked to cancer progression and migration. It is particularly valuable for researchers investigating the role of PAK1 in various biological processes and disease models. -
PAK4 Inhibitor
CZh226 hydrochloride is a selective inhibitor of PAK4, demonstrating an IC50 of 18 nM with a remarkable selectivity ratio of 346-fold for PAK4 over PAK1. Despite its low oral bioavailability, it serves as a valuable tool for investigating tumorigenic pathways in colorectal cancer and melanoma when combined with prodrug PAK4-IN-1 to enhance absorption and metabolic stability. This compound provides significant insights into PAK4's role in cancer biology and therapeutic potential. -
PAK4 Degrader
PAK4-IN-6 is a selective degrader of PAK4 (p21-activated kinase 4), functioning through targeted protein degradation mechanisms. This compound serves as a valuable tool in the synthesis of proteolysis-targeting chimeras (PROTACs) and has potential applications in cancer research and therapeutic development. Its ability to modulate PAK4 levels makes it instrumental in studying signaling pathways and cellular processes involving this kinase. -
PAK1 Inhibitor
AZ13711265 is a potent and selective inhibitor of PAK1, displaying IC50 values of 0.58 nM for PAK1 and 0.11 µM for phosphorylated PAK1 (pPAK1). Its low lipophilicity and clearance profile make AZ13711265 suitable as an in vivo probe for studying PAK1's role in various biological processes. This compound is particularly relevant for research applications in cancer, providing insights into PAK1-mediated signaling pathways and therapeutic targeting. -
PAK4 Inhibitor
PAK4-IN-1 is a potent and selective inhibitor of PAK4, demonstrating significant anti-tumor efficacy in in vivo models. This compound remains stable under acidic and neutral conditions, making it suitable for various experimental settings. PAK4-IN-1 is primarily utilized in cancer research to investigate the role of PAK4 in tumor progression and to explore potential therapeutic strategies targeting this pathway. -
PAK1 Inhibitor
ZINC194100678 is a potent PAK1 inhibitor, demonstrating an IC50 value of 8.37 μM. This compound effectively inhibits the proliferation of MDA-MB-231 breast cancer cells, making it a valuable tool for cancer research. Its mechanism of action provides insights into the role of PAK1 in tumor growth and offers potential avenues for therapeutic intervention in cancer treatments. -
PAK4 Inhibitor
KY-04031 is a selective PAK4 inhibitor with an IC50 of 0.79 μM, effectively targeting the ATP-binding pocket of PAK4. This compound has demonstrated significant anti-tumor activity by inhibiting both tumor cell growth and invasion. KY-04031 is suitable for research applications focusing on cancer biology and the elucidation of PAK4's role in tumor progression. -
PAK inhibitor
KT D606 is a selective PAK kinase family inhibitor with an IC50 value of 4 μM. This compound effectively inhibits the proliferation of cancer cells harboring oncogenic RAS mutations, making it a valuable tool for research on RAS/PAK1-induced malignancies. Its specificity for PAK kinases provides insights into the molecular mechanisms underlying oncogenic signaling pathways. -
PAK4 Inhibitor
KY-04045 is a specific inhibitor of PAK4, demonstrating an IC50 value of 8.7 μM. This compound plays a crucial role in the study of cancer biology by inhibiting PAK4 activity, which is implicated in tumorigenesis and cancer progression. KY-04045 is valuable for research aimed at developing novel therapeutics targeting PAK4-mediated pathways in cancer. -
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. -
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.
