tubulin β

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

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

Vindoline is an indole alkaloid that exhibits antimitotic activity by inhibiting microtubule assembly.

Epothilone B (EPO 906) is a compound isolated from the myxobacterium Sorangium cellulosum. Similar to paclitaxel, patupilone induces microtubule polymerization and stabilizes microtubules against depolymerization conditions. In addition to promoting tubulin polymerization and stabilization of microtubules, this agent is cytotoxic for cells overexpressing P-glycoprotein, a characteristic that distinguishes it from the taxanes. Patupilone may cause complete cell-cycle arrest.

Epothilone A (Epo A) is a microtubule-stabilizing agent with EC0.01 of 2 μM.

Cynaropicrin, a sesquiterpene lactone found in artichoke (Cynara scolymus), has anti-hepatitis C and trypanosome activity and inhibits NF-κB activation. Cynaropicrin disrupts microtubulin- and c-Myc-related signaling and induces parthanatos-type cell death in multiple myeloma.

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

7a-Hydroxyfrullanolide possesses anticancer properties and can reduce the polymerization of α- and β-tubulins. It preferentially binds to β-tubulin over α-tubulin. Additionally, 7a-Hydroxyfrullanolide induces a DNA damage response, causing cell arrest in the G2/M phase. This compound is a eucalyptolide sesquiterpene lactone (SL) and can be extracted from Asteraceae family flowering plants.

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.

SKLB050 is derived from the natural chalcone small molecule millepachine (MIL), which is extracted from the plant [Millettia pachycarpa]. SKLB050 exhibits potential antitumor activity both in vitro and in vivo. Biochemical and cellular assays indicate that SKLB050 binds directly and irreversibly to β-tubulin.