Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Cardiogenic Molecule
Shz-1, a small cardiogenic molecule, primarily targets cardiac-specific gene expression. It has been shown to induce the expression of key cardiac markers, including sarcomeric tropomyosin in P19CL6 cells and Nkx2.5 in mouse models. Additionally, Shz-1 activates the axolotl TPM4 promoter, driving ectopic expression in C2C12 cells. This compound is valuable for research in cardiac development and regenerative medicine. -
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. -
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. -
α5β1 Integrin Agonist
α5β1 integrin agonist-1 is a potent agonist of the α5β1 integrin, exhibiting an EC50 of 1.5 nM. This compound also inhibits α4β1 integrin activity with an IC50 of 2.99 μM, as demonstrated in Jurkat/VCAM-1 adhesion assays. α5β1 integrin agonist-1 induces concentration-dependent apoptosis and activates the caspase 3/7 pathway in α5β1 integrin-expressing K562 cancer cells. This reagent is suitable for investigations into cancer biology, particularly in studies focusing on integrin-mediated signaling pathways. -
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. -
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. -
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.
