Microtubule/Tubulin

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  1. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.
  2. Vinorelbine is the first 5??NOR semi-synthetic vinca alkaloid. It is obtained by semi-synthesis from alkaloids extracted from the rosy periwinkle, Catharanthus roseus.
  3. microtubule inhibitor

    Nocodazole is a microtubule inhibitor; inhibits mitosis. Also inhibits autophagosome-lysosome fusion.
  4. microtubule inhibitor

    Ixabepilone is an epothilone B analog
  5. Arp2/3 complex inhibitor

    CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.
  6. Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
  7. Docetaxel trihydrate, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
  8. Microtubule Associated inhibitor

    Paclitaxel (Taxol) is a mitotic inhibitor that stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division.
  9. microtubule stabilizer

    Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity.
  10. Microtubule Associated inhibitor

    Cabazitaxel is a semi-synthetic derivative of a natural taxoid. Cabazitaxel in combination with prednisone is a treatment option for hormone-refractory prostate cancer following docetaxel-based treatment
  11. Microtubule Associated inhibitor

    Docetaxel (Taxotere) is an antineoplastic agent that acts by disrupting the microtubular network in cells that is essential for mitotic and interphase cellular functions.
  12. Eribulin mesylate is the mesylate salt of a synthetic analogue of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity.
  13. Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin, and also shows inhibition of antibody-drug conjugates (ADCs) activity.
  14. microtubule-targeting agent

    Fosbretabulin disodium is the disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combretum caffrum) with potential vascular disrupting and antineoplastic activities.
  15. Cevipabulin (TTI-237), an antimicrotubule agent, is a small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from the action of other vinca alkaloid compounds, TTI-237 specifically binds to tubulin at the vinca site, and promotes the polymerization of tubulin into microtubules.
  16. Colchicine is an inhibitor of microtubules by specific binding to tubulin.
  17. Microtubule Associated inhibitor

    Epothilone B is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis.
  18. Combretastatin A4 is an antitumor, antiangiogenic and antimetastatic agent, in vitro and in vivo. Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
  19. microtubule depolymerizing agent

    Ansamitocin P-3 is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
  20. SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.
  21. tubulin polymerization inhibitor

    Crolibulin, also known as EPC2407 and crinobulin, is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
  22. Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
  23. Microtubule/Tubulin Inhibitor

    SSE15206 is a pyrazolinethioamide derivative that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.
  24. microtubule destabilizing agents

    Tubulysin family of secondary metabolites are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizing agents with IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties. Tubulysins have limited therapeutic utility due to severe toxicity, so Tubulysins are ideal candidates to be incorporated into molecule drug conjugate (SMDC) delivery system.
  25. maytansinoid microtubular inhibitor

    DM1-SMe is a potent maytansinoid microtubular inhibitor and an unconjugated DM1 as a mixed disulfide with thiomethane to cap its sulfhydryl group.
  26. antitubulin agent

    MMAF-Ome, an antitubulin agent, belongs to ADC.
  27. 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel (a microtubule stabilizing agent; enhances tubulin polymerization) derivative with improved pharmacological features.
  28. microtubule depolymerizing agent

    Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
  29. microtubulin inhibitor

    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
  30. anti-tubulin agent

    Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.
  31. 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C; 7-Epitaxotere) is a impurity of docetaxel.
  32. 7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).
  33. 10-Oxo Docetaxel (Docetaxel Impurity 1) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
  34. Microtubule-Targeting Agent

    ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
  35. tubulin polymerization inhibitor

    BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
  36. Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
  37. Arp2/3 complex inhibitor

    CK-869 is an Actin-Related Protein 2/3 (ARP2/3) complex inhibitor, with an IC50 of 7 μM.
  38. Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.
  39. β-tubulin polymerization inhibitor

    Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
  40. Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
  41. tubulin inhibitor

    Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.
  42. Tubulin assembly inhibitor

    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity.
  43. tubulin polymerization inhibitor

    Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
  44. β-tubulin polymerization inhibitor

    Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  45. microtubule inhibitor

    Rosabulin is a potent microtubule inhibitor, with anti-cancer activities.
  46. tubulin inhibitor

    altobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.
  47. cytotoxic tubulin modifier

    Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates. Auristatin F inhibits cell division by blocking the polymerisation of tubulin.
  48. cytotoxic tubulin modifier

    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
  49. Dolastatin 10 (DLS 10) is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.
  50. microtubule-disrupting agent

    Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types.

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