microtubule

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Colchicine is an orally active natural alkaloid that acts by inhibiting microtubule polymerization (IC50 = 3 nM) and as a competitive antagonist of the α3 glycine receptor. It possesses broad anti-inflammatory, immunosuppressive, and antifibrotic activities, can inhibit NLRP3 inflammasome activation to prevent NSAID-induced small intestine injury, holds potential for gouty arthritis and rheumatoid arthritis research, and is commonly used to establish Alzheimer’s disease models.

4'-Demethylepipodophyllotoxin (DMEP) is a potent inhibitor of microtubule assembly.

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.

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.

Ansamitocin p-3 (Maytansinol isobutyrate) is an inhibitor of microtubule with IC50 of 3.4 μM for tubulin polymerization.

Curvulin is the active metabolite isolated from Paraphoma sp. VIZR 1.46. Curvularin inhibits iNOS expression and microtubule assembly.

Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.

Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is the first natural product steroid identified to have these cellular effects,with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.

Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.

L-Clausenamide is an alkaloid extracted from the leaves of the yellow bark (Clausena lansium (Lour) skeels) and can be used to improve cognitive function. L-Clausenamide inhibits beta-amyloid (Aβ) toxicity and prevents the formation of neurofibrillary tangles by inhibiting tau phosphorylation. L-Clausenamide has neuroprotective activity and can be used to modulate stimuli triggered by Aβ25-35. L-Clausenamide can be used to study neurological disorders like Alzheimer's disease.

Podofilox ((+)-Shikonin) is a lignan (LIGNANS) found in PODOPHYLLIN resin from the roots of PODOPHYLLUM plants. It is a potent spindle poison, toxic if taken internally, and has been used as a cathartic. It is very irritating to skin and mucous membranes, has keratolytic actions, has been used to treat warts and keratoses, and may have antineoplastic properties, as do some of its congeners and derivatives.

Mebendazole (Mebenvet) is a hedgehog inhibitor, used as an antihelminthic.

Griseofulvin (Fulvicin) is an antifungal agent used in the treatment of TINEA infections.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

Combretastatin A4 (CA4) is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM).

Jasplakinolide(Jaspamide), a naturally occurring cyclic peptide from marine sponges, is a potent inducer of actin polymerization.Jasplakinolide exhibits antifungal and antitumor activity and stabilizes pre-existing actin filaments. Jasplakinolide competitively binds to F-actin with the ghost pen cyclic peptide and has a Kd value of 15 nM for F-actin.

Ceratamine A, an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., functions as a microtubule-stabilizing agent with cytotoxic effects against human cancer cell lines.

Cytochalasin A, a cell-permeable fungal toxin and oxidized derivative of cytochalasin B, is an inhibitor of HIV-1 protease (IC50 = 3 μM). It inhibits actin polymerization, interferes with microtubule assembly by reacting with sulfhydryl groups, and serves as an antibiotic and bactericidal active agent.

Tubulysin D is a tetrapeptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and displays potent antitumor activity.

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

Colcemid (NSC-3096) is a microtubule polymerization inhibitor, with the main target being Tubulin and an IC50 of 2.4 μM. Colcemid can induce apoptosis and can be used in the research of tumors and embryo cloning.

Cephalomannine (Baccatin III) is a taxol derivative obtained from Taxus yunnanensis with antitumor activity.