Microtubule/Tubulin
Microtubules are major dynamic structural components in cells. They are important in the development and maintenance of cell shape, in cell reproduction and division, in cell signaling, and in cellular movement. Microtubules are the target of a diverse group of anticancer drugs, most of which are derived from natural products. Microtubules are highly dynamic polymers of heterodimers of a and b tubulin, arranged parallel to a cylindrical axis to form tubes of 25 nm diameter that may be many mm long. Polymerization of microtubules occurs by a nucleation-elongation mechanism in which the formation of a short microtubule ‘nucleus‘ is followed by elongation of the microtubule at its ends by the reversible, noncovalent addition of tubulin dimers. Microtubules are not simple equilibrium polymers. They exhibit complex polymerization dynamics that use energy provided by the hydrolysis of GTP, and these dynamics are crucial to their cellular functions. A large number of chemically diverse substances bind to tubulin or microtubules and inhibit cell proliferation by acting on microtubules. Many of these have become drugs that are highly useful in the treatment of various forms of cancer or are currently in clinical trials. Microtubules are the target of a diverse group of anticancer drugs, most of which are derived from natural products.
References
1.Jordan MA. Curr Med Chem Anticancer Agents. 2002;2(1):1–17.
References
1.Jordan MA. Curr Med Chem Anticancer Agents. 2002;2(1):1–17.
Cytoskeleton/Cell Adhesion Molecules
Microtubule/Tubulin
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Dolastatin 10
catalog no : M29578
cas no: 110417-88-4
Dolastatin 10 is a potent antimitotic peptide that inhibits tubulin polymerization. -
Tubulin inhibitor 24
catalog no : M28918
cas no: 2415761-65-6
Tubulin inhibitor 24 is a potent inhibitor that can inhibit tubulin polymerization. -
LP-261
catalog no : M28789
cas no: 915412-67-8
LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. -
MAP4343
catalog no : M28721
cas no: 511-26-2
Map4343 is a 3-methyl ether derivative of pregnenolone. Map4343 binds to microtubule associated protein 2 (MAP2) in vitro and stimulates tubulin polymerization, resulting in enhanced neurite extension and protection of neurons from neurotoxic agents. -
TTBK1-IN-2
catalog no : M28535
cas no: 2765453-51-6
TTBK1-IN-2 is an inhibitor of Tau-Tubulin kinase (TTBK1) with IC50s of 0.24 and 4.22 μM. TTBK1-IN-2 reduces TDP-43 phosphorylation both in cell cultures and the spinal cord of transgenic TDP-43 mice.