Catalog No.
Product Name
Application
Product Information
Citations
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Antimicrotubule Chemotherapy Agent
Estramustine phosphate is an estradiol analog that functions as an orally active antimicrotubule chemotherapy agent. By binding to microtubule-associated proteins (MAPs) and/or tubulin, it depolymerizes microtubules, disrupting mitosis and promoting cell death through apoptosis. This compound is predominantly utilized in cancer research, particularly for studies related to prostate cancer. -
IDO/Tubulin Inhibitor
IDO/Tubulin-IN-2 is a potent inhibitor targeting both indoleamine 2,3-dioxygenase (IDO) and tubulin. This compound exhibits significant anticancer activity, demonstrated by its effect on various cell lines, including U87, HepG2, A549, HCT-116, and LO2, with IC50 values of 0.43, 0.036, 0.041, 0.095, and 1.04 μM, respectively. IDO/Tubulin-IN-2 is valuable for research applications in cancer biology, particularly in elucidating mechanisms of tumorigenesis and therapeutic resistance. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-61 is a potent tubulin polymerization inhibitor that disrupts microtubule dynamics, leading to the destruction of the microtubule skeleton. This compound effectively blocks the cell cycle at the G2/M phase, inducing apoptosis and inhibiting cancer cell migration and colony formation. In preclinical studies, Tubulin polymerization-IN-61 demonstrates significant antitumor activity in the 4T1 xenograft model, highlighting its potential for cancer research and therapeutic applications. -
Tubulin Polymerization Inhibitor
Tubulin Inhibitor 33 is a tubulin polymerization inhibitor that disrupts microtubule assembly in a dose-dependent manner, with an IC50 of 9.05 μM. This compound exhibits significant antitumor activity by promoting apoptosis in cancer cells. Tubulin Inhibitor 33 is a valuable reagent for research focusing on cancer biology and the mechanisms of tumorigenesis. -
Tubulin/MMP Inhibitor
Tubulin/MMP-IN-2 is a dual inhibitor targeting both tubulin and matrix metalloproteinases (MMPs). It effectively inhibits tubulin polymerization, leading to induced apoptosis in cancer cells. Additionally, Tubulin/MMP-IN-2 demonstrates inhibitory activity against MMP-2, MMP-3, and MMP-9, with IC50 values of 24.95 μM, 31.60 μM, and 22.37 μM, respectively. This compound is valuable for research focused on cancer biology and therapeutic development. -
Tubulin Ligand
SL-3-19 is a tubulin ligand that inhibits microtubule assembly, leading to significant antitumor activity against esophageal squamous cell carcinoma (ESCC) in both in vitro and in vivo models. This compound induces G2/M phase cell cycle arrest and apoptosis, while also disrupting tumor vascularization. SL-3-19 serves as a valuable reagent for research focused on ESCC and related malignancies. -
Microtubule/Tubulin Inhibitor
Maytansine is a highly potent microtubule-targeting agent that disrupts microtubule dynamics, leading to mitotic arrest and apoptosis in tumor cells. It exerts cytotoxic effects at subnanomolar concentrations and serves as the cytotoxic payload component in several antibody–drug conjugates (ADCs) used for targeted cancer therapy. -
Cx43 modulator
Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43) that prevents the uncoupling of Cx43-mediated gap junction communication and restores intercellular connectivity under acute metabolic stress. As a potent and stable antiarrhythmic peptide (AAP), Rotigaptide shows strong potential for the investigation of cardiac arrhythmias, particularly atrial fibrillation. - Estramustine is an antineoplastic agent that exerts antimitotic activity by depolymerizing microtubules through binding to tubulin 1. It inhibits mitosis in DU 145 prostate cancer cells with an IC50 of approximately 16 μM and induces mitotic arrest in prostate tumor xenograft models, making it a valuable compound for prostate cancer research and therapy.
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Microtubule/Tubulin Inhibitor
EAPB 02303 is a microtubule-disrupting agent that inhibits microtubule dynamics, leading to mitotic arrest and impaired spindle assembly. This disruption induces apoptosis and contributes to its antitumor activity. EAPB 02303 also demonstrates potent synergistic effects with Paclitaxel at lower concentrations, enhancing its potential in combination cancer therapies. -
MAPK/ERK/PKC/PKA Activator
Gardenin A is an orally active synthetic polymethoxyflavone (PMF) analogue with neurotrophic properties, promoting neurite outgrowth and neuronal differentiation. It enhances neuritogenesis through activation of the MAPK/ERK, PKC, and PKA pathways, independent of TrkA and CREB signaling. Additionally, Gardenin A exhibits sedative, anxiolytic, antidepressant, and anticonvulsant effects, making it a promising compound for neurological and neuropsychiatric research. -
Apoptosis activator
Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB. -
CBSI inhibitor
MY-673 is a colchicine binding site inhibitor (CBSI) that disrupts microtubule dynamics by inhibiting tubulin polymerization. In addition to its antimitotic effects, MY-673 suppresses the ERK signaling pathway, which leads to modulation of SMAD4 protein expression within the TGF-β/SMAD signaling axis. These combined actions result in potent inhibition of cancer cell proliferation and migration, and the induction of apoptosis, both in vitro and in vivo. MY-673 holds promise as a therapeutic candidate for targeting cancers driven by aberrant microtubule dynamics and dysregulated TGF-β/ERK signaling. -
HDAC6 inhibitor
T-518 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 36 nM for human HDAC6. It is capable of crossing the blood–brain barrier, making it suitable for central nervous system applications. T-518 is particularly useful in tauopathy research, where HDAC6 inhibition may modulate tau pathology and neurodegenerative processes. -
Tubulin/AKT1 Inhibitor
Tubulin/AKT1-IN-1 is an inhibitor of tubulin polymerization and AKT pathway activation. This compound demonstrates significant inhibition of proliferation and metastasis in H1975 cells, along with a modest induction of apoptosis. Tubulin/AKT1-IN-1 is particularly relevant for research in non-small cell lung cancer (NSCLC), providing a valuable tool for studying therapeutic strategies against this malignancy. -
Tubulin Inhibitor
Tubulin-IN-55 is a potent tubulin inhibitor that disrupts the PI3K/Akt signaling pathway in cancer cells. This compound exhibits broad-spectrum anti-proliferative effects against various tumor cell lines, including HeLa, HCT116, 4T1, A549, H1299, and MDA-MB231. Tubulin-IN-55 induces G2/M phase arrest and promotes apoptosis, while also inhibiting tumor cell migration and invasion. In vivo studies demonstrate significant antitumor efficacy in orthotopic autologous transplantation models, making Tubulin-IN-55 a valuable tool for cancer research. -
Microtubule Depolymerizing Agent
Naphthazarin is a microtubule depolymerizing agent that exhibits significant biological activity in various research applications. It has been shown to improve motor function and decrease neuroinflammation in mouse models of Parkinson's disease. Additionally, Naphthazarin induces apoptosis, autophagy, and cell cycle arrest in tumor cells. Its ability to trigger erythrocyte apoptosis further underscores its potential utility in studies of tumors and neurodegenerative diseases. -
PAK2 Inhibitor
PQA-18 is a selective inhibitor of PAK2, exhibiting an inhibitory concentration (IC50) of 10 nM. This compound demonstrates significant immunosuppressive effects by downregulating the production of pro-inflammatory cytokines including IL-2, IL-4, IL-6, and TNF-α. PQA-18 also affects regulatory T cell populations and reduces immunoglobulin production in response to T cell-dependent antigens, contributing to the alleviation of dermatitis in murine models. Its application may extend to research in autoimmune diseases and immunology. -
Tubulin/CDC5L Inhibitor
Tubulin/CDC5L-IN-1 is a dual inhibitor targeting both tubulin and CDC5L. It inhibits cancer cell proliferation and induces G2/M phase arrest, facilitating apoptosis and reactive oxygen species (ROS) production in affected cells. Additionally, Tubulin/CDC5L-IN-1 demonstrates antiangiogenic properties, making it a valuable tool for cancer research, particularly in studies related to colon carcinoma. -
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. -
Microtubule Inhibitor
Microtubule Inhibitor 2 acts as a selective microtubule disruptor, inducing cell death via ferroptosis. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying microtubule-targeted therapies. -
Microtubule Inhibitor
Microtubule Inhibitor 8 (MP-HJ-1b) targets microtubule dynamics, acting as a potent disruptor of microtubule processing. This compound initiates cell death through the ferroptosis pathway and exhibits significant anti-tumor activity. It serves as an essential tool for research in cancer biology and therapeutic development focused on targeting microtubules. -
Tubulin Inhibitor
Tubulin Inhibitor 30 is a potent tubulin polymerization inhibitor, exhibiting an IC50 of 0.52 μM. This compound disrupts microtubule dynamics, leading to the induction of ferroptosis in various cell types. It serves as a valuable tool for research on cancer biology and therapeutic applications targeting the cytoskeletal network. -
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. -
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. -
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
Polatuzumab vedotin is an antibody-drug conjugate that targets CD79b and functions primarily as a microtubule inhibitor. This compound consists of a humanized anti-CD79b IgG1 monoclonal antibody conjugated to monomethyl auristatin E (MMAE), a potent agent that disrupts microtubule dynamics. Its unique mechanism makes Polatuzumab vedotin a valuable tool for studying large B-cell lymphomas (LBCL) and exploring therapeutic approaches in related malignancies. Researchers can leverage its targeted delivery system for enhanced therapeutic efficacy in the context of cancer research. -
Tubulin ADC
Anetumab ravtansine is a potent antibody-drug conjugate (ADC) that specifically targets tubulin via a conjugation of a human anti-mesothelin antibody to the maytansinoid tubulin inhibitor DM4. This compound demonstrates significant antitumor activity, which correlates with mesothelin expression levels in patient-derived xenograft tumor models. Anetumab ravtansine is primarily used in cancer research, particularly in studies focusing on targeted therapies for mesothelin-expressing tumors. -
Microtubule Disassembly Inhibitor
10-Acetyl docetaxel is a microtubule disassembly inhibitor known for its antimitotic activity. As an analog of Docetaxel, this compound effectively disrupts microtubule dynamics, making it a valuable reagent in cancer research. Its mechanism of action can be leveraged to study cellular processes related to mitosis and the development of anticancer therapies. -
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. -
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.
