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Catalog No.
Product Name
Application
Product Information
Citations
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kinesin Eg5 inhibitor
Litronesib (Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5. -
inhibitor of tubulin polymerization
4-Oxo-4-HPR is an inhibitor of tubulin polymerization, inducing marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines. It is also a fenretinide metabolite. -
Myosin II Inhibitor
Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function. Blebbistatin blocks cell migration. -
Tubulin Inhibitor
Demecolcine is a potent tubulin inhibitor that effectively disrupts microtubule polymerization, exhibiting an IC50 value of 2.4 μM. By binding to tubulin dimers, Demecolcine exerts anti-mitotic effects, hindering cellular division. This compound is primarily utilized in research related to inflammatory disorders and various cancer pathways, making it valuable for studies focused on cell cycle regulation and targeted therapies. -
Microtubule Acetylation Inhibitor
GM-90257 is a potent microtubule acetylation inhibitor that directly binds to α-tubulin. By preventing the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue, GM-90257 disrupts microtubule dynamics, leading to apoptotic cell death. It downregulates Bcl-2 and activates key apoptotic pathways, including JNK and PARP. This compound demonstrates significant anticancer activity in breast cancer models, making it a valuable tool for research in cancer therapeutics and microtubule biology. -
Microtubule Inhibitor
MPT0B214 is a potent microtubule inhibitor that targets the colchicine binding site of tubulin, effectively preventing tubulin polymerization. This compound induces apoptosis via a mitochondrial/caspase 9 dependent pathway and exhibits significant cytotoxic effects across a range of human tumor cell lines. MPT0B214 is suitable for applications in cancer research, allowing for further exploration of microtubule dynamics and therapeutic strategies. -
Tubulin Polymerization Inhibitor
Trilexium is a potent tubulin polymerization inhibitor that effectively disrupts microtubule integrity. This compound promotes the expression of p21 protein and triggers apoptotic pathways, demonstrating significant anti-cancer activities across various cell lines. Trilexium holds promise for research applications focused on cancer biology and novel therapeutic strategies targeting microtubule dynamics. -
Tubulin Inhibitor
Tubulin polymerization-IN-68 is a potent tubulin inhibitor that disrupts tubulin polymerization, thereby destabilizing the microtubule network within cells. This compound induces apoptosis by upregulating PARP-1 and caspase-3 expression, showcasing significant anticancer properties. Tubulin polymerization-IN-68 demonstrates effective inhibition of HepG2 cells with an IC50 of 93 nM and substantially reduces the growth of HepG2 xenograft tumors in nude mice when administered orally, making it a valuable tool for cancer research. -
Tubulin Inhibitor
STK899704 is a potent tubulin polymerization inhibitor that demonstrates broad-spectrum antitumor activity across various cancer cell lines, with IC50 values between 0.2 and 1.0 μM. By disrupting mitotic spindle formation, STK899704 induces G2/M phase cell cycle arrest and decreases cell migration in HT29 cells through the FAK-MEK-ERK signaling axis, leading to reduced expression and activity of MMP-2 and MMP-9. This compound activates caspases 3, 7, 8, and 9, resulting in PARP cleavage and subsequent apoptosis, alongside triggering cellular senescence via the p53 pathway. STK899704 is applicable in research focusing on skin cancer, lung cancer, colon cancer, and other 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. -
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. -
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. -
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. -
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. -
Tubulin Inhibitor
Antitumor agent-68 is a potent tubulin inhibitor that demonstrates significant anticancer activity, with IC50 values of 3.6 μM and 3.8 μM against HeLa and MCF-7 cancer cell lines, respectively. This compound exhibits strong reactive oxygen species (ROS) and DPPH radical scavenging activity in a dose-dependent manner, making it relevant for oxidative stress research. Antitumor agent-68 also features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, facilitating advancements in chemical biology applications. -
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. -
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. -
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. -
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. -
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/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 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. -
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.
