Microtubule/Tubulin

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  1. 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.
  2. 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.
  3. microtubule assembly inhibitor

    4-Demethylepipodophyllotoxin is a potent inhibitor of microtubule assembly.
  4. Microtubule Associated inhibitor

    ABT-751 is an antimitotic agent, inhibits microtubule polymerization, binds to β-tubulin on the colchine site; blocks cell cycle at G2M phase and induces apoptosis.
  5. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
  6. Chloroxine is an antibacterial drug useful for dandruff and seborrheic dermatitis.
  7. Colchicine is an inhibitor of microtubules by specific binding to tubulin.
  8. Microtubule Inhibitor

    CYT997 is a novel anti-cancer vascular disrupting agent (VDA). In vitro, CYT997 is shown to potently inhibit the proliferation of vascular endothelial growth factor-stimulated human umbilical vein endothelial cells (IC(50) 3.7 ?? 1.8 nM) and cause significant morphological changes at 100 nM, including membrane blebbing.
  9. 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.
  10. Microtubule Associated inhibitor

    Epothilone A acts by stabilising microtubule formation at the taxol binding site and causes cell cycle arrest at the G2/M transition, leading to cytotoxicity.
  11. 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.
  12. Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.
  13. Tubulin inhibitor

    Vincristine is a mitotic inhibitor, and is used in cancer chemotherapy.
  14. Microtubule Associated inhibitor

    Vinflunine Tartrate is a tartrate salt of vinflunine that destabilizes microtubules with an IC50 of 18.8 nM and interferes with the dynamics of microtubules during cell division.
  15. 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.
  16. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.
  17. microtubule inhibitor

    Ixabepilone is an epothilone B analog
  18. Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
  19. 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
  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. 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.
  22. 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.
  23. 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.
  24. 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.
  25. microtubule inhibitor

    Nocodazole is a microtubule inhibitor; inhibits mitosis. Also inhibits autophagosome-lysosome fusion.
  26. 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.
  27. microtubule dynamics inhibitor

    Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer.
  28. Microtubule Associated inhibitor

    CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 uM, significant selectivity over KSP.
  29. Arp2/3 inhibitor

    CK-636 is a Arp2/3 complex inhibitor. CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation.
  30. Hec1 imhibitor

    INH1 is a Hec1 inhibitor. It binds Hec1, inhibiting its association with Nek2 and kinetochores.
  31. Hec1 Inhibitor

    INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
  32. Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin.
  33. microtubule stabilizer

    Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity.
  34. VcMMAE is an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
  35. Tubulin inhibitor

    D-64131 is a novel inhibitor of tubulin polymerization that inhibits tumor cell proliferation in vitro (IC50 = 74 nM).
  36. Microtubule polymerization inhibitor

    Cucurbitacin B, a natural triterpenoid is well-known for its strong anticancer activity, and recent studies showed that the compound inhibits JAK/STAT3 pathway. Also it is an potent Microtubule polymerization inhibitor
  37. 7-Epi 10-Desacetyl Paclitaxel is a derivative of Paclitaxel, which is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
  38. 7-xylosyltaxol is a taxol derivative, Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.
  39. Docetaxel trihydrate, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
  40. Tubulin inhibitor

    Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate; Mc-MMAD is a protective group (maleimidocaproyl) -conjugated MMAD.
  41. Tubulin inhibitor

    MMAD, a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
  42. Tubulin inhibitor

    Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulin inhibitor (MMAD), Vc-MMAD is an antibody drug conjugate.
  43. Microtubule Disruptor

    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in ??III-tubulin-overexpressing cell lines.
  44. 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.
  45. tau protein aggregation inhibitor

    TRx 0237 (LMT) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
  46. tubulin polymerization inhibitor

    Crolibulin, also known as EPC2407 and crinobulin, is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
  47. Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
  48. 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.
  49. 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.
  50. Microtubule inhibitor

    VCP-Eribulin consists the ADCs linker (VCP) and Eribulin. Eribulin is a mechanistically unique microtubule inhibitor for cancer. VCP-Eribulin is an Eribulin-based drug for antibody conjugates.

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