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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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
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 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. -
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. -
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.
