microtubules

Terflavoxate is a novel, orally active, semisynthetic statin microtubule inhibitor commonly used in combination with capecitabine. Terflavoxate is used in cancer research.

Eribulin mesylate (E7389 mesylate) (E7389 mesylate) inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. Eribulin mesylate (E7389 mesylate) is a microtubule targeting agent that is used in the treatment of metastatic breast cancer.

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2 M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

Cemadotin free base(LU103793 free base) is a novel anti-limiting peptide , an analog of Dolastatin 15, a naturally occurring cytotoxic peptide that blocks mitosis and inhibits microtubules (tubulin) with a Ki of 1 μM. Cemadotin is used in research against cancer.

OSIP-486823(CP248) is a novel and potent microtubule disruptor with affinity for both protein kinase G (PKG) and microtubules.

XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. It triggers apoptosis and has anti-tumor effects

Vincristine sulfate is an alkaloidal natural product that binds to microtubule proteins and inhibits the formation of microtubules, thereby inhibiting mitosis in tumor cells. Vincristine sulfate is used as a microtubule destabilizing agent in research studies for the treatment of hematologic neoplasms such as leukemias and lymphomas, as well as in studies related to sarcomas in children.

Eribulin (B1939) is a nonpaclitaxel microtubule kinetic inhibitor with anticancer activity that inhibits polymerization of microtubule protein subunits by preventing lengthening and shortening of microtubules during cell division.Eribulin is used in the study of metastatic breast cancer and solid tumors.

Myoseverin, an inducer of the reversible fission of multinucleated myotubes into mononucleated fragments, affecting the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.

Tasidotin (also known as ILX-651) is an orally active synthetic derivative targeting microtubules, derived from the marine depsipeptide dolastatin-15.

Larotaxel (XRP9881) is a taxane analogue with anticancer activity that promotes tubulin assembly and stabilizes microtubules, inducing apoptosis. It crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, making it useful for studying breast and bladder cancer.

Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

20-O-Demethyl-AP3 is a secondary metabolite derived from Ansamitocin P-3 [a macrocyclic antitumor antibiotic] that exerts its therapeutic effects by inhibiting microtubules.

Disermolide is a polyketide natural product found to stabilize microtubules. Disermolide was found to be a potent inhibitor of tumor cell growth in several MDR cancer cell lines.

Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].

Vinflunine Tartrate, a uniquely fluorinated vinca alkaloid, exhibits mitotic-arresting and tubulin-interacting properties.

Desmethyl-HD-800 is a PET precursor of preparing radiolabel [11C]HD-800, a high affinity brain penetrant PET tracer for imaging microtubules.

Non-hydrolyzable AMP analog. Kir6 (KATP) channel blocker. Inhibits fast axonal transport and stabilizes the interaction of membranous organelles with microtubules. Brady (1985) A novel brain ATPase with properties expected for the fast axonal transport motor. Nature 317 73 PMID:2412134 |Yount et al (1971) Adenylyl imidodiphosphate, an adenosine triphosphate analog containing a P-N-P linkage. Biochemistry 10 2484 PMID:4326768 |Hehl and Neumcke (1994) KATP channels of mouse skeletal muscle: mechanism of channel blockage by AMP-PNP. Eur.Biophys.J. 23 231 PMID:7805625

Green fluorescent taxol derivative. Used for microtubule imaging. Binds microtubules with high affinity (Ka ~ 107M-1). Excitation/emission maximum λ ~ 496/526 nm. Lillo et al (2002) Location and properties of the Tax. binding center in microtubules: a picosecond laser study with fluorescent taxoids. Biochemistry. 41 12436 PMID:12369834 |Diaz et al (2000) Molecular recognition of Tax. by microtubules. Kinetics and thermodynamics of binding of fluorescent Tax. derivatives to an exposed site. J.Biol.Chem. 275 26265 PMID:10818101

Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].

Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2 M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).