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.

Cevipabulin (TTI-237) is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

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

CID-663143 inhibits cancer cell growth and shows microtubule-binding activity.

Erbulozole (R 55104) is a potent synthetic microtubule inhibitor with anti-invasive, anti-tumor, and radiosensitizing activities that induces Wernicke's encephalopathy-like neurotoxicity.

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.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

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.

Docetaxel (RP-56976), a semi-synthetic analog of paclitaxel, is a microtubule depolymerization inhibitor (IC50=0.2 μM) that attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

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.

Albendazole (SKF-62979) is used as a drug indicated for the treatment of a variety of worm infestations.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

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.

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

BRD9876 is a selective inhibitor of MM1S growth.

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.

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

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood-brain barrier permeable microtubule-disrupting agent with potent and broad-spectrum cytotoxic activities and significant anticancer efficacy in human MX-1 breast cancer and various mouse xenograft cancer models.

Eribulin mesylate (E7389 mesylate) belongs to natural product derivatives and is a microtubule-targeted anticancer agent, functioning as a microtubule dynamics inhibitor that suppresses tubulin polymerization through tubulin binding, with cell permeability. This drug is used for the treatment of metastatic breast cancer.

Auristatin F is an effective inhibitor of microtubule and vascular damaging agent. Auristatin F can be used in antibody-drug conjugates.

Pironetin binds to α-tubulin and is an effective inhibitor of microtubule polymerization. It also has cell cycle arrest and antitumor activity. Pironetin is an α/β unsaturated lactone isolated from Streptomyces species.

v Rosabulin (STA 5312) is an orally active microtubule inhibitor with potency. Rosabulin inhibits microtubule assembly and has broad-spectrum antitumor activity.