Cytoskeleton

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  1. Integrin Antagonist

    TR-14035 is a dual antagonist of α4β7 and α4β1 integrins.
  2. 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.
  3. 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.
  4. microtubule assembly inhibitor

    4-Demethylepipodophyllotoxin is a potent inhibitor of microtubule assembly.
  5. 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.
  6. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
  7. Chloroxine is an antibacterial drug useful for dandruff and seborrheic dermatitis.
  8. Colchicine is an inhibitor of microtubules by specific binding to tubulin.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. KSP Inhibitor

    Ispinesib (SB-715992) is a potent inhibitor of kinesin spindle protein, a kinesin motor protein essential for the formation of a bipolar mitotic spindle and cell cycle progression through mitosis.
  14. ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
  15. Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.
  16. KSP Inhibitor

    SB 743921, a second generation KSP inhibitor, is a highly potent and active therapeutic in preclinical models of cancer.
  17. Tubulin inhibitor

    Vincristine is a mitotic inhibitor, and is used in cancer chemotherapy.
  18. 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.
  19. 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.
  20. KSP inhibitor

    KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5) with potential antineoplastic activity.
  21. Mps1 inhibitor

    AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). It interferes with chromosome alignment and overrides spindle assembly checkpoint and also Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.

  22. Myosin activator

    CK-1827452 is a selective cardiac specific myosin activator.
  23. Mps1 inhibitor

    Mps1-IN-1 is a highly potent and selectibe Mpsl inhibitor with IC50 of 367 nM; >1000-fold selectivity relative to the 352 member kinase panel with the major exceptions of Alk and Ltk.
  24. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.
  25. CENP-E inhibitor

    GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E).
  26. microtubule inhibitor

    Ixabepilone is an epothilone B analog
  27. gap-junction modulator

    Tonabersat is a novel benzopyran derivative that blocks the cortical spreading depression proposed to be associated with migraine attacks.
  28. VCAM-1 antagonist

    CDP323 is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 binding to ??4-integrins
  29. Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
  30. 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
  31. PAK4 inhibitor

    PF-3758309 is a small-molecule p21-activated kinase inhibitor inhibiting oncogenic signaling and tumor growth.
  32. MLCK inhibitor

    ML 7 hydrochloride is a selective inhibitor of myosin light chain kinase (MLCK).
  33. Kinesin-5(KIF11) inhibitor

    Monastrol is a potent, cell permeable non-tubulin-interacting mitosis inhibitor. Monastrol blocks mitosis (IC5N/A = 14 μM) by binding to the mitotic kinesin Eg5, a motor protein required for spindle bipolarity.
  34. TTK inhibitor

    CFI-402257, a pyrazolopyridin derivative, has been found to be a TTK inhibitor that could influence chromosome segregation and induce cell death so that is significant in anticancer studies.
  35. 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.
  36. Integrin inhibitor

    Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.
  37. Integrin inhibitor

    Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.
  38. PAK inhibitor

    FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nM, PAK2 IC50= 13 nM, PAK3 IC50= 19 nM).
  39. 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.
  40. 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.
  41. allosteric PAK1 inhibitor

    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
  42. Dynamin inhibitor

    Dynasore is a non-competitive inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity
  43. α4β1/α4β7 integrin antagonist

    Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).
  44. 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.
  45. Pyrintegrin is a cell-permeable small molecule that promotes human embryonic stem cell (hESC) survival by > 30-fold.
  46. Integrin Inhibitor

    A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 value of 20 nM and 25 nM, respectively.
  47. 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.
  48. PKC inhibitor

    GF 109203X is a potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM).
  49. microtubule inhibitor

    Nocodazole is a microtubule inhibitor; inhibits mitosis. Also inhibits autophagosome-lysosome fusion.
  50. 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.

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