Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. - 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. -
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. -
Ras Activator
Methylophiopogonanone B is a homoisoflavonoid that serves as a Ras activator. Isolated from the root of Ophiopogon japonicus, it exhibits potent antioxidant properties. This compound enhances GTP-Rho levels and activates the Rho signaling pathway, thereby inducing morphological changes in cells, such as actin cytoskeletal reorganization, dendrite retraction, and stress fiber formation. It is a valuable reagent for research into cellular signaling and structural dynamics. -
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. -
Anti-Tubulin Agent
DPQZ is an anti-tubulin agent that disrupts microtubule dynamics, leading to inhibition of cell separation and inducing cell cycle arrest at the G2/M phase. Additionally, DPQZ triggers caspase-dependent apoptosis in HSC-3 cells through the inhibition of Ras/Raf signaling and the activation of MAP kinase pathways. This compound is relevant for research applications in studying oral cancer biology 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. -
Microtubule-stabilizing Agent
Simotaxel is a microtubule-stabilizing agent that acts as an orally active derivative of the taxane class. It binds to β-tubulin, promoting tubulin polymerization with an EC₅₀ of 0.9 μM, while inhibiting tubulin depolymerization and causing cell cycle arrest in the G₂-M phase. Additionally, Simotaxel disrupts mitotic spindle formation and activates the caspase-dependent apoptotic pathway. This compound is particularly relevant for research into Paclitaxel- and Docetaxel-resistant solid tumors, demonstrating inhibitory effects on cell lines sensitive to these treatments. -
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. -
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. -
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/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. -
Tubulin Polymerization Inhibitor
SB-216 is a tubulin polymerization inhibitor that penetrates the blood-brain barrier. It demonstrates significant antitumor activity by inhibiting tumor cell proliferation and migration, as well as inducing apoptosis and cell cycle arrest. With favorable in vivo metabolic stability and low toxicity, SB-216 is suitable for research applications focused on various tumors, including melanoma, although its oral bioavailability is limited. -
Microtubule Stabilizer
Taccalonolide E is a microtubule stabilizer that enhances microtubule polymerization and stability, leading to disruption of mitotic spindle formation. This compound effectively induces apoptosis in various cancer cell types by activating pathways associated with cell cycle arrest. Taccalonolide E is useful for research involving cancer biology, specifically in studies targeting microtubule dynamics and apoptotic mechanisms. -
Tubulin Polymerization Inhibitor
MPT0B014 is a potent tubulin polymerization inhibitor that disrupts microtubule dynamics. This compound has been shown to induce apoptosis in cancer cells, making it a valuable tool for studying cancer biology and therapeutic interventions. MPT0B014 is suitable for research focused on cancer treatment strategies and cellular response to microtubule-targeting agents. -
Tubulin inhibitor
Tubulin inhibitor 11 is a potent inhibitor of tubulin that acts by targeting the colchicine binding site on tubulin. It effectively inhibits tubulin polymerization, resulting in mitotic blockade and the induction of apoptosis. This compound is a valuable tool for research applications investigating cell division, cancer biology, and the mechanisms of drug resistance. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-56 is a potent inhibitor of tubulin polymerization that targets the colchicine binding site. This indazole derivative effectively induces cell cycle arrest and promotes cellular apoptosis. Additionally, Tubulin polymerization-IN-56 reduces cell migration, resulting in significant inhibition of tumor growth in vivo and demonstrating its potential for cancer research applications. -
Tubulin Polymerization Inhibitor
Thiocolchicine is a tubulin polymerization inhibitor that exhibits enhanced biological properties compared to its parent compound, colchicine. With an IC50 of 2.5 µM, it competitively binds to tubulin with a Ki of 0.7 µM, effectively disrupting microtubule dynamics and inducing cell apoptosis. Thiocolchicine serves as a valuable cytotoxin in antibody-drug conjugate (ADC) technology, making it an important reagent for cancer research and therapeutic development. -
Microtubulin polymerization Inhibitor
MY-1442 is a microtubulin polymerization inhibitor that functions by targeting colchicine binding sites on tubulin. This compound exhibits significant anticancer activity, effectively inducing apoptosis in MGC-803 cells. Additionally, MY-1442 has been shown to inhibit cell migration, making it a valuable reagent for research applications in cancer biology and cell motility studies. -
Tubulin Inhibitor
FC-116 is a potent tubulin inhibitor that disrupts microtubule dynamics, leading to the inhibition of colorectal cancer (CRC) cell proliferation. It demonstrates significant activity with IC50 values of 4.52 nM in HCT116 cells and 18.69 nM in CT26 cells. By inducing endoplasmic reticulum stress and generating excess reactive oxygen species (ROS), FC-116 promotes mitochondrial damage and apoptosis in CRC cells. This compound also exhibits substantial anti-tumor effects in vivo, making it a valuable reagent for colorectal cancer research. -
Tubulin Inhibitor
Taltobulin trifluoroacetate is a potent tubulin inhibitor that targets microtubule dynamics. This synthetic analogue of hemiasterlin effectively inhibits the polymerization of purified tubulin, leading to disrupted microtubule organization within cells. Taltobulin trifluoroacetate induces mitotic arrest and apoptosis, making it a valuable compound for research in cancer biology and studies focused on overcoming P-glycoprotein-mediated drug resistance. -
Microtubule-destabilizing Agent
Antiproliferative agent-23 is a microtubule-destabilizing agent that disrupts the tubulin-microtubule system. It induces apoptosis through a mitochondrion-dependent mechanism by downregulating Bcl-2, while upregulating Bax and Cyt c proteins, thereby activating the caspase cascade. Additionally, antiproliferative agent-23 triggers reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells via the PERK/ATF4/CHOP signaling pathway, demonstrating significant anti-tumor activity. This compound is suitable for research applications aimed at understanding cancer biology and therapeutic interventions. -
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
Tubulysin B is a potent microtubule destabilizing agent that selectively inhibits tubulin polymerization. Naturally derived from the myxobacteria Archangium geophyra and Angiococcus disciformis, it exhibits high cytotoxicity with IC50 values in the picomolar range across various cancer cell lines, including those exhibiting multidrug resistance. This compound is valuable for studies focused on cancer biology, specifically in elucidating mechanisms of cell cycle arrest and apoptosis. -
Src/Tubulin Inhibitor
KX2-361 is an inhibitor of Src-kinase and tubulin polymerization. This compound exhibits significant anti-tumor activity and induces apoptosis in glioblastoma (GBM) cells. With good oral bioavailability and the ability to cross the blood-brain barrier in murine models, KX2-361 is a valuable tool for investigating Src-related signaling pathways and therapeutic strategies in cancer research. -
Tubulin/JAK2-IN-1 inhibitor, Antitumor
Tubulin/JAK2-IN-1 is a dual inhibitor targeting Janus kinase 2 (JAK2) and microtubules, exhibiting potent antitumor activity. This compound demonstrates significant antiproliferative effects against various cancer cell lines, making it a valuable tool in cancer research. Its dual mechanism of action supports investigations into therapies that disrupt cell division and signaling pathways in malignancies. -
Tubulin Inhibitor
Antiproliferative agent-30 is a tubulin inhibitor that disrupts tubulin assembly and effectively inhibits FLT3 and Abl1 activity. This compound demonstrates impressive antiproliferative effects against various cancer cell lines, exhibiting IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM for HCT-116, K562, and MV-4-11 cells, respectively. Additionally, Antiproliferative agent-30 shows potential in targeting acute myeloid leukemia (AML) cells with FLT3-ITD-TKD mutations, highlighting its significance in cancer research and potential therapeutic applications. -
Microtubule Inhibitor
MPT0B002 is a potent microtubule inhibitor that targets tubulin polymerization, leading to significant anticancer effects. This compound induces apoptosis and effectively arrests the cell cycle at the G2/M phase. MPT0B002 is useful in various cancer research applications, providing insights into microtubule dynamics and the mechanisms of tumor cell proliferation. -
Tubulin/VEGFR Inhibitor
Tubulin/VEGFR-2-IN-2 is an orally active inhibitor targeting tubulin and VEGFR-2, exhibiting IC50 values of 3.27 μM and 0.09 μM, respectively. This compound demonstrates significant antitumor activity by enhancing reactive oxygen species generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Additionally, Tubulin/VEGFR-2-IN-2 possesses anti-angiogenic effects, impairing endothelial cell migration, invasion, and tube formation in vitro. It effectively suppresses angiogenesis, tumor growth, and metastasis in vivo, making it a valuable tool for research involving non-small cell lung cancer, breast cancer, gastric cancer, and lymphoma. -
Tubulin polymerization Inhibitor
Tubulin polymerization-IN-11 is a potent inhibitor of tubulin polymerization with an IC50 value of 3.4 μM. It demonstrates significant antiproliferative activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. Mechanistically, Tubulin polymerization-IN-11 reduces the expression levels of cyclin B1, phosphorylated cdc2, and Bcl-2 while increasing the expression of cleaved PARP, making it valuable for research in cancer biology and cell cycle regulation.
