Discodermolide  (Synonyms: NVP-XAA-296; XAA 296)

Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a K_i of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel (HY-B0015) to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research^[1][2][3].

593.79

C₃₃H₅₅NO₈

127943-53-7

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• [1]. Altmann KH. Microtubule-stabilizing agents: a growing class of important anticancer drugs. Curr Opin Chem Biol. 2001 Aug;5(4):424-31.  [Content Brief]

  [2]. Kowalski RJ, et al. The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and inhibits the growth of paclitaxel-resistant cells. Mol Pharmacol. 1997 Oct;52(4):613-22.  [Content Brief]

  [3]. Hung DT, et al. (+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks taxol binding and results in mitotic arrest. Chem Biol. 1996 Apr;3(4):287-93.  [Content Brief]