Cytoskeleton

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  1. Tubulin Polymerization Inhibitor

    Tubulin polymerization-IN-26 is a potent inhibitor of microtubulin polymerization, specifically targeting the colchicine binding site with an IC50 value of 4.64 μM. This compound exhibits cytotoxic effects by inducing apoptosis and impeding cellular migration and metastasis. It serves as a valuable tool for research applications focused on lung cancer and related studies in tumor dynamics.
  2. Microtubule inhibitor

    IMB5046 is a potent microtubule inhibitor that disrupts microtubule dynamics, leading to cell cycle arrest at the G2/M phase and subsequent apoptosis. This compound exhibits significant anti-tumor activity, making it a valuable reagent for cancer research and therapeutic studies focused on cell proliferation and apoptosis mechanisms.
  3. Microtubule Depolymerization Agent

    PBOX-15 is a microtubule depolymerization agent that functions by disrupting tubulin polymerization, leading to the destabilization of microtubules. This compound induces apoptosis in tumor cells, making it a valuable tool in cancer research. PBOX-15 is utilized to investigate the mechanisms of microtubule dynamics and to evaluate potential therapeutic strategies for malignancies.
  4. αβ-Tubulin Inhibitor

    αβ-Tubulin-IN-1 is a powerful inhibitor targeting αβ-Tubulin. This compound effectively induces cell cycle arrest at the G2/M phase and promotes efficient apoptosis in cancer cells. Additionally, αβ-Tubulin-IN-1 inhibits tumor cell migration and metastasis, demonstrating significant antitumor efficacy in a dose-dependent manner. It serves as a valuable tool for research into cell cycle regulation and cancer therapeutics.
  5. PAK4 Inhibitor

    PF-3758309 hydrochloride is a potent and reversible ATP-competitive inhibitor targeting PAK4, with a Kd of 2.7 nM and a Ki of 18.7 nM. This compound is effective in inhibiting anchorage-independent growth and inducing apoptosis, while also promoting cytoskeletal remodeling and suppressing cellular proliferation. PF-3758309 hydrochloride is valuable in research applications aimed at understanding PAK4's role in cancer and other diseases associated with dysregulated cell growth.
  6. Tubulin Ligand

    SL-1-73 is a potent tubulin ligand that disrupts microtubule assembly, leading to G2/M phase cell cycle arrest and apoptosis in tumor cells. Its antitumor activity has been demonstrated both in vitro and in vivo against esophageal squamous cell carcinoma (ESCC), as well as other malignancies. SL-1-73 is a valuable tool for investigating the mechanisms underlying ESCC and exploring potential therapeutic options targeting microtubule dynamics.
  7. Inhibitor of Tubulin Polymerization

    DPP-21 is a potent inhibitor of tubulin polymerization, with an IC50 value of 2.4 μM. This compound exhibits significant anti-proliferative effects in various cancer cell lines, including IC50 values of 0.38 nM in HCT116, 11.69 nM in B16, 5.37 nM in HeLa, 9.53 nM in MCF7, 8.94 nM in H23, and 9.37 nM in HepG2. DPP-21 effectively arrests the cell cycle at the G2/M phase, leading to increased apoptosis in tumor cells, as demonstrated by a decrease in Bcl-2 levels and an upregulation of the pro-apoptotic protein Bax.
  8. Microtubule Disruptor

    STX140 is an orally active microtubule disruptor that targets the stabilization of microtubules to promote cell cycle arrest. This compound induces apoptosis in hormone-independent PC-3 prostate cancer cell lines, demonstrating significant anti-tumor properties. STX140 is also noted for its anti-angiogenic activity, making it a valuable tool for cancer research and therapeutic development.
  9. Tubulin Inhibitor

    3-(3-Phenoxybenzyl)amino-β-carboline is a potent inhibitor of tubulin, specifically targeting αβ-tubulin heterodimers. This compound has been shown to induce G2/M phase cell cycle arrest and subsequent apoptosis in cancer cells. Its significant anticancer activity makes it a valuable tool for research applications aimed at understanding tumor biology and developing novel therapeutic strategies.
  10. Sulfonamides Antimitotic Compounds/Tubulin Binders Agent

    ABT-751 hydrochloride is a potent sulfonamide antimitotic compound that functions primarily as a tubulin binder. By binding to the colchicine site on β-tubulin, it prevents tubulin aggregation, leading to cell cycle arrest in the G2/M phase and subsequent apoptosis. Additionally, ABT-751 hydrochloride induces autophagy through the inhibition of the AKT/mTOR signaling pathway. This compound demonstrates significant antiproliferative effects against a range of cancer cell types, including lung, gastric, colon, and breast cancer.
  11. HI5

    IDO/Tubulin Inhibitor

    HI5 is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO) and tubulin, demonstrating an IC50 of 70 nM in HeLa cells. It effectively reduces kynurenine production, thereby promoting T cell activation and proliferation. Additionally, HI5 interferes with tubulin polymerization and migration, induces G2/M phase cell cycle arrest, and triggers apoptosis through a mitochondrial-dependent pathway, leading to increased reactive oxidative stress. HI5 is suitable for research in anticancer applications.
  12. Tubulin Polymerization Inhibitor

    Tubulin polymerization-IN-24 is a potent inhibitor of tubulin polymerization. This compound effectively inhibits the proliferation of MCF-7 breast cancer cells, inducing apoptosis and causing cell cycle arrest at the G2/M phase. Additionally, Tubulin polymerization-IN-24 enhances the rate of GTP hydrolysis while inhibiting microtubule assembly, making it a valuable tool for research into cancer biology and cellular dynamics.
  13. Tubulin Polymerization Inhibitor

    Tubulin polymerization-IN-86 is a potent inhibitor of tubulin polymerization that targets the colchicine binding sites on microtubulin, effectively disrupting the microtubule cytoskeleton. This compound demonstrates significant anti-proliferative activity against various cancer cell lines and induces mechanisms such as cell cycle arrest and apoptosis. Additionally, it inhibits cell migration and invasion, contributing to reduced long-term survival of cancer cells. Tubulin polymerization-IN-86 also exhibits efficacy in inhibiting tumor growth in murine models, making it a valuable tool for research in melanoma and related studies.
  14. β-microtubulin Inhibitor

    Tubulin inhibitor 42 (Compound 14b) primarily targets β-microtubulin, exhibiting dose-dependent inhibition with an IC50 of 3.5 µM. This compound disrupts microtubule dynamics, leading to cancer cell cycle arrest in the G2/M phase and triggering apoptosis. Additionally, Tubulin inhibitor 42 demonstrates significant inhibitory effects on angiogenesis, both in vitro and in vivo, ultimately suppressing vascularization and tumor progression.
  15. Tubulin Inhibitor

    SKLB0565 is a potent tubulin inhibitor that demonstrates significant anti-proliferative effects in colorectal carcinoma (CRC) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. This compound induces G2/M phase cell cycle arrest and triggers mitochondria-mediated intrinsic apoptosis. Additionally, SKLB0565 effectively inhibits cell migration and disrupts tube formation in human umbilical vein endothelial cells (HUVECs), making it a valuable tool for cancer research and the study of tumor angiogenesis.
  16. Microtubule Modulator

    NMK-TD-100 is a microtubule modulator that binds to tubulin, effectively inhibiting tubulin polymerization with an IC50 of 17.5 µM. This compound disrupts mitosis and leads to a decrease in mitochondrial membrane potential (MMP). Additionally, NMK-TD-100 demonstrates significant anti-proliferative activity against HeLa cells, with an IC50 of 1.42 µM, causing cell cycle arrest at the G2/M phase and inducing apoptosis. Its applications include studying microtubule dynamics and exploring potential cancer therapies.
  17. Microtubulin Inhibitor

    Microtubulin-IN-1 is a selective inhibitor of microtubulin that targets the colchicine-binding site, leading to disruption of microtubule integrity and upregulation of p53. It demonstrates significant antiproliferative activity across various cancer cell lines, with IC50 values of 2.4 nM for NCI-H460, 1.6 nM for BxPC-3, and 2.07 nM for HT-29. Microtubulin-IN-1 effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in NCI-H460 cells, making it a valuable tool for cancer research.
  18. Tubulin Inhibitor

    Tubulin polymerization-IN-6 is a potent tubulin polymerization inhibitor with an IC50 of 1.09 μM. This compound effectively impairs cell migration and tube formation, playing a significant role in anti-angiogenesis. In vivo studies demonstrate that Tubulin polymerization-IN-6 substantially inhibits tumor growth in HT29 xenograft models using Balb/c nude mice, making it a valuable reagent for cancer research.
  19. VEGFR-2/β-tubulin Inhibitor

    VEGFR-2-IN-22 is a dual inhibitor targeting VEGFR-2 and β-tubulin polymerization, demonstrating an IC50 of 19.82 nM against VEGFR-2. This compound promotes apoptosis, making it a valuable tool for studying angiogenesis and cancer biology. Its mechanism of action provides insights into vascular endothelial growth factor pathways and their role in tumor progression.
  20. Tubulin Polymerization Inhibitor

    Tubulin polymerization-IN-17 is a potent inhibitor of tubulin polymerization, effectively disrupting microtubule dynamics. This compound induces depolymerization of tubulin, leading to apoptosis in cancer cells and inhibiting their migratory capabilities. Tubulin polymerization-IN-17 is valuable for research focused on cancer biology and therapies targeting microtubule dynamics.
  21. Tubulin polymerization inhibitor

    Tubulin polymerization-IN-84 is a selective inhibitor of tubulin polymerization that targets the colchicine-binding site, exhibiting an IC50 of 10.9 μM. This compound demonstrates significant antiproliferative effects against various cancer cell lines, including Jurkat, B16-F10, HCT116, and MDA-MB-231, with IC50 values of 60 nM, 380 nM, 138 nM, and 1.054 μM, respectively. Tubulin polymerization-IN-84 induces G2/M-phase arrest and promotes apoptosis in B16-F10 cells, while also suppressing tumor growth in a B16-F10 melanoma model. Additionally, it enhances anti-tumor immunity in conjunction with PD-L1 monoclonal antibodies, making it a valuable reagent for research in T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer studies.
  22. Integrin ligand

    VSLRGDTRG is a synthetic peptide derived from cadherin 17 (CDH17) that functions as a ligand for the α2β1 integrin. This peptide promotes the conformational activation of β1 integrin via the RGD motif, leading to enhanced cell adhesion and increased phosphorylation of FAK and ERK1/2. VSLRGDTRG is applicable in cancer research, specifically in studies involving tumors expressing CDH17, including colon and pancreatic cancers, where it may aid in understanding mechanisms of tumor proliferation and metastasis.
  23. microtubule assembly inhibitor

    4-Demethylepipodophyllotoxin is a potent inhibitor of microtubule assembly.
  24. 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.
  25. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
  26. Chloroxine is an antibacterial drug useful for dandruff and seborrheic dermatitis.
  27. 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.
  28. 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.
  29. 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.
  30. Microtubule Inhibitor

    NPI-2358 is a synthetic analog of NPI-2350, a natural product isolated from Aspergillus sp., which depolymerizes microtubules in A549 human lung carcinoma cells.
  31. Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.
  32. KSP Inhibitor

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

    Vincristine is a mitotic inhibitor, and is used in cancer chemotherapy.
  34. 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.
  35. KSP inhibitor

    KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5) with potential antineoplastic activity.
  36. microtubule targeting agent

    Eribulin (E7389) is a microtubule targeting agent that is used in the treatment of metastatic breast cancer.
  37. MPS1 kinase inhibitor

    BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
  38. MPS1 kinase inhibitor

    Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
  39. Mps1 inhibitor

    Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.
  40. microtubule-disrupting agent

    Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities.
  41. Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  42. MPS1 inhibitor

    NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
  43. PAK inhibitor

    GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
  44. mitotic/tubulin inhibitor

    D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
  45. MPS1 inhibitor

    CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.
  46. tubulin polymerisation inhibitor

    Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
  47. αVβ3 integrin inhibitor

    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  48. auristatin microtubule inhibitor

    PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue.
  49. microtubule assembly and microtubule dynamics inhibitor

    Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15, as an inhibitor of microtubule assembly and microtubule dynamics.
  50. α4 integrin receptor inhibitor

    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.

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