Catalog No.
Product Name
Application
Product Information
Citations
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Antitubulin Agent
MMAF hydrochloride (Monomethylauristatin F) is a potent inhibitor of tubulin polymerization, primarily functioning as an antitumor agent. It demonstrates significant cytotoxic activity and is commonly utilized as a key component in antibody-drug conjugates (ADCs), including Vorsetuzumab mafodotin and SGN-CD19A. This reagent is essential for research applications focused on cancer therapeutics and the development of targeted drug delivery systems. -
Microtubule/Tubulin Inhibitor
DM4-SMe is a potent tubulin inhibitor, primarily targeting microtubules to disrupt cytoskeletal functions. As a metabolite of antibody-maytansinoid conjugates, it serves as a cytotoxic component in antibody-drug conjugates. DM4-SMe exhibits significant biological activity, demonstrating an IC50 of 0.026 nM against KB cells. Additionally, this highly toxic metabolite undergoes oxidation and detoxification by human liver microsomes, which may influence its pharmacokinetic profile in biological systems. -
Antitubulin Agent
MMAF sodium (Monomethylauristatin F sodium) is a potent antitubulin agent that functions as an inhibitor of tubulin polymerization. It exhibits significant cytotoxic activity, making it a crucial component in the development of antibody-drug conjugates (ADCs), including Vorsetuzumab mafodotin and SGN-CD19A. This compound is widely employed in cancer research to explore strategies for targeted therapy and to enhance the efficacy of therapeutic agents against various malignancies. -
Tubulin Polymerization Inhibitor
Fmoc-MMAF-OMe is a tubulin polymerization inhibitor that features an Fmoc protecting group. The active component, MMAF, serves as a cytotoxic agent in antibody-drug conjugates (ADCs), making it critical for cancer research. Its ability to disrupt microtubule dynamics positions Fmoc-MMAF-OMe as a valuable tool for studying various cancer pathways and evaluating potential therapeutic strategies. -
Microtubule Inhibitor
S-methyl DM1 is a thiomethyl derivative of Maytansine and functions as a microtubule inhibitor. It binds to tubulin with a dissociation constant (Kd) of 0.93 μM, effectively inhibiting microtubule polymerization and potently suppressing microtubule dynamic instability. Due to its mechanism of action, S-methyl DM1 exhibits significant anticancer properties, making it a valuable reagent for research in cancer biology and therapeutics. -
Microtubule/Tubulin Inhibitor
DM3-SMe is a maytansine derivative that acts as a potent tubulin inhibitor. This compound exhibits remarkable cytotoxic activity in vitro, with an IC50 of 0.0011 nM, making it suitable for various research applications, particularly in the development of antibody-drug conjugates (ADCs). DM3-SMe can be conjugated to antibodies via disulfide or stable thioether bonds, enhancing the targeted delivery of cytotoxic agents in cancer therapy research. -
Anti-microtubule Toxins
Tubulysin C is a potent anti-microtubule toxin that targets tubulin, effectively disrupting microtubule dynamics. This compound exhibits significant cytotoxic activity in mammalian cells, including those resistant to multiple drugs, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule polymerization, resulting in cell cycle arrest and apoptosis. It is valuable for research in cancer biology and the development of targeted therapies. -
Microtubule Disrupting Agent
AGD-0182 is a microtubule disrupting agent that functions by binding to tubulin and inhibiting microtubule polymerization. As a synthetic analogue of the natural compound Dolastatin 10, AGD-0182 serves as a valuable tool for studying microtubule dynamics. In addition to its primary function, it features an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with alkyne-containing molecules. This dual functionality makes AGD-0182 suitable for diverse applications in chemical biology and bioconjugation research. -
Microtubule/Tubulin Inhibitor
Tubulysin IM-2 is a potent microtubule and tubulin inhibitor that disrupts microtubule polymerization, leading to cell cycle arrest and apoptosis in tumor cells. This compound serves as a valuable component in antibody-drug conjugates (ADCs) by imparting cytotoxic effects and enhancing therapeutic efficacy. It is particularly useful in cancer research where targeting microtubule dynamics is crucial for investigating tumor progression and treatment responses. -
Anti-microtubule Toxins
Tubulysin IM-3 is an anti-microtubule toxin that inhibits tubulin polymerization, disrupting microtubule dynamics. Its primary mechanism involves binding to tubulin, which effectively impedes cellular mitosis and triggers apoptotic pathways. This compound serves as a valuable cytotoxic agent in antibody-drug conjugate (ADC) synthesis, enhancing the therapeutic efficacy of targeted cancer treatments. -
Microtubule Stabilizer
Flutax-2 is a fluorescent derivative of Paclitaxel, functioning as a microtubule stabilizer through specific binding to polymerized αβ-tubulin dimers. This reagent is ideal for imaging microtubules in live cells, isolated cytoskeletons, and certain parasitic organisms, with excitation and emission wavelengths of 496 nm and 526 nm, respectively. Its high sensitivity enables researchers to investigate microtubule dynamics and cellular processes in real-time applications. -
Microtubule/Tubulin Inhibitor
Bis-ANS dipotassium is a fluorescent probe that targets tubulin, acting as a microtubule inhibitor. It exhibits a binding affinity with tubulin characterized by a Kd of 2 μM. This compound serves as a potent biphasic modulator of protein liquid-liquid phase separation (LLPS), promoting LLPS at low concentrations while suppressing it at elevated concentrations. Its unique properties make it valuable for studying microtubule dynamics and phase separation mechanisms in cellular processes. -
Tubulin Polymerisation Inhibitor
Tubulin Polymerization-IN-38 is a tubulin polymerization inhibitor that disrupts microtubule dynamics, leading to enhanced apoptosis in cancer cells. As an analogue of Tubulysin, it demonstrates powerful anticancer activity and serves a pivotal role in research applications focusing on cancer treatment and drug discovery. This compound can also be utilized as an antibody-drug conjugate (ADC) cytotoxin, facilitating the synthesis of targeted therapies for oncology research. -
Tubulin Polymerization Inhibitor
Tubulysin D is a potent tubulin polymerization inhibitor that disrupts microtubule dynamics. This highly cytotoxic compound, derived from the myxobacteria Archangium geophyra and Angiococcus disciformis, exhibits significant activity against mammalian cells, including those with multidrug resistance, with IC50 values in the low nanomolar range. By preventing microtubule assembly, Tubulysin D induces cell cycle arrest and apoptosis, making it a valuable tool for cancer research and studies on microtubule-targeting therapies. -
Tubulin Inhibitor
Bi-Mc-VC-PAB-MMAE is a drug-linker conjugate that targets tubulin through a potent microtubule destabilizer, MMAE. The compound combines the ADC linker Bi-Mc-Val-Cit-PAB with MMAE to inhibit microtubule polymerization, effectively disrupting cellular mitotic processes. This reagent is primarily used in antibody-drug conjugate (ADC) research for its potential applications in targeted cancer therapies. -
Tubulin Inhibitor
PC5-VC-PAB-MMAE is a potent tubulin inhibitor linked to an antibody-drug conjugate (ADC) via the PC5-VC-PAB linker. This compound demonstrates significant biological activity by disrupting microtubule dynamics, thereby inhibiting cell proliferation. It serves as a valuable tool for research applications focused on cancer therapy and the study of microtubule-targeting agents. -
Microtubule Inhibitor
Lisavanbulin dihydrochloride is a microtubule inhibitor that functions as a prodrug for the active compound Avanbulin. It demonstrates significant antitumor activity, particularly in tumors with elevated levels of end-binding protein 1, by targeting tumor cell proliferation and modulating the tumor microenvironment through the reduction of tumor microvasculature. Additionally, Lisavanbulin dihydrochloride activates the spindle assembly checkpoint, leading to cell cycle arrest, cell death, or aberrant chromosome segregation. This compound is relevant for research focused on diffuse large B cell lymphoma (DLBCL) and glioblastoma. -
Microtubule Inhibitor
Lisavanbulin is a prodrug of the microtubule-targeting agent Avanbulin, functioning as an effective antitumor agent with the ability to penetrate the blood-brain barrier. It primarily targets tumor cell proliferation and modifies the tumor microenvironment by reducing tumor microvasculature. Additionally, Lisavanbulin activates the spindle assembly checkpoint, leading to cell cycle arrest, cell death, or abnormal chromosome segregation. This reagent is relevant for research applications in diffuse large B cell lymphoma (DLBCL) and glioblastoma. -
Microtubule Inhibitor
Combretastatin A-1 acts as a microtubule polymerization inhibitor by binding to the colchicine-binding site on tubulin. This compound disrupts microtubule dynamics, leading to the deactivation of AKT and inhibition of the Wnt/β-catenin signaling pathway. Combretastatin A-1 is recognized for its anti-tumor and anti-vascular properties, making it a valuable tool for cancer research and the study of vascular dynamics. -
Microtubule Inhibitor
Combretastatin A-1 phosphate tetrasodium is a microtubule inhibitor that targets the colchicine-binding site of tubulin, leading to disruption of microtubule polymerization. This compound has been shown to inhibit the Wnt/β-catenin signaling pathway through AKT deactivation mediated by tubulin depolymerization. Its key biological activities include anti-tumor and anti-vascular effects, making it a valuable reagent for cancer research and studies involving microtubule dynamics. -
PAK4 Inhibitor
GL-1196 is a potent inhibitor of PAK4, a serine/threonine kinase involved in cancer cell proliferation and invasion. This compound effectively inhibits PAK4-mediated signaling pathways leading to decreased proliferation and invasiveness in gastric cancer cells. GL-1196 disrupts the PAK4/c-Src/EGFR/Cyclin D1 and CDK4/6 axis, which results in the reduction of filamentous pseudopodia formation and promotes cell elongation in SGC7901 and BGC823 cell lines. Its applications in anti-cancer research make it a valuable tool for studies targeting gastric cancer progression. -
PAK1 Degrader
BJG-05-039 is a selective degrader of PAK1, formed by the conjugation of NVS-PAK1-1 and Lenalidomide. This compound effectively induces degradation of PAK1, resulting in the inhibition of MEK S298 and ERK phosphorylation. BJG-05-039 demonstrates notable anti-proliferative effects in PAK1-dependent cell lines, making it a valuable tool for research applications focused on PAK1-related signaling pathways and cancer biology. -
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.
