Cytoskeleton

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  1. CENP-E inhibitor

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

    Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
  3. 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.
  4. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.
  5. MTF-1 inhibitor

    LOR-253 is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1).
  6. 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.
  7. microtubule inhibitor

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

    Ixabepilone is an epothilone B analog
  9. 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).
  10. 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).
  11. Myosin activator

    CK-1827452 is a selective cardiac specific myosin activator.
  12. 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.
  13. 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.
  14. αvβ3 integrin inhibitor

    Cyclo (-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin.
  15. 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.

  16. Inhibits integrin binding to RGD motifs

    RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins.
  17. CaMKII inhibitor

    KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.
  18. Dynamin inhibitor

    Dyngo-4a is a potent dynamin inhibitor with IC50 of 0.38 uM, 1.1uM, and 2.3 uM for DynI (brain), DynI (rec), and DynII (rec), respectively.
  19. Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
  20. Gap junction blocker

    Gap 26 is a connexin mimetic peptide, corresponding to residues 63-75 of connexin 43, which is a gap junction blocker.
  21. 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.
  22. VCAM-1 antagonist

    CDP323 is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 binding to ??4-integrins
  23. PAK inhibitor

    FRAX486 is a small-molecule PAK inhibitor.
  24. Docetaxel trihydrate, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
  25. 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.
  26. microtubule stabilizer

    Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity.
  27. MLCK inhibitor

    ML 7 hydrochloride is a selective inhibitor of myosin light chain kinase (MLCK).
  28. Gap junction blocker

    Gap 27 is a peptide derived from connexin 43 that is a selective gap junction blocker.
  29. 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
  30. 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.
  31. 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.
  32. 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.
  33. α1β1 inhibitor

    Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.
  34. DRP1 inhibitor

    Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.
  35. Dynamin inhibitor

    Dynasore is a non-competitive inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity
  36. 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.
  37. 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.
  38. Colchicine is an inhibitor of microtubules by specific binding to tubulin.
  39. 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.
  40. Gap Junction Modifier

    GAP-134 , a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability.
  41. 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.
  42. Pyrintegrin is a cell-permeable small molecule that promotes human embryonic stem cell (hESC) survival by > 30-fold.
  43. 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.
  44. gap-junction modulator

    Tonabersat is a novel benzopyran derivative that blocks the cortical spreading depression proposed to be associated with migraine attacks.
  45. PAK4 inhibitor

    PF-3758309 is a small-molecule p21-activated kinase inhibitor inhibiting oncogenic signaling and tumor growth.
  46. 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.
  47. 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.
  48. Integrin receptor antagonist

    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  49. PKA, PKG, Casein Kinase I and II inhibitor

    A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).
  50. 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.

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