microtubule/tubulin

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.

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) inhibits tubulin polymerization (IC50 = 4 μM) and has anti-mitotic effects.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

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.

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

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

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.

Nocodazole (Oncodazole) is a reversible inhibitor of microtubule polymerization and an inhibitor of Bcr-Abl. Nocodazole has antitumor activity, blocks the cell cycle and induces apoptosis.

Vinorelbine ditartrate (KW-2307) is a natural alkaloid and an anti-mitotic agent. Vinorelbine ditartrate has anti-tumor activity, inhibiting cell proliferation and inducing apoptosis.

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

Colchicine (Colcin) is a natural product that is an inhibitor of microtubule polymerization (IC50=3 nM) and blocks microtubule polymerization by binding to microtubule proteins. Colchicine can be used in the treatment of ventilation and rheumatic diseases.

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.

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

DM4 (Ravtansine) can be used in the preparation of antibody drug conjugate and it is an antitubulin agent. It can inhibit cell division.

Colcemid (NSC-3096) is an inhibitor of microtubule polymerization. It used to study embryonic cloning.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

NQTrp is an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects.

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.

Vindesine sulfate (Desacetyl Vinblastine amide) is a vinca alkaloid which is a synthetic derivative of vinblastine, binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.

MMAF (MonoMethyl auristatin F), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.

VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity.