Microtubule/Tubulin

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  1. Dolastatin 10 Synthesis Intermediate

    (S)-Dolaphenine hydrochloride serves as a synthesis intermediate for Dolastatin 10, a potent antineoplastic agent. This compound acts by inhibiting tubulin polymerization, thereby disrupting microtubule dynamics crucial for cell division. Research applications include the investigation of cancer therapeutics and the exploration of novel chemotherapeutic strategies.
  2. Taxane Derivative

    10-Deacetyltaxol, a taxane derivative, primarily targets tubulin polymerization in microtubule dynamics. It effectively promotes the assembly of tubulin and inhibits depolymerization induced by cold conditions or calcium ions in vitro. This compound displays significant cytotoxicity against human glial and neuroblastoma cell lines, making it valuable for research in cancer biology and therapeutics.
  3. Microtubule/Tubulin

    MAP4343 is a 3-methylether derivative of pregnenolone that targets microtubules by binding to microtubule-associated protein 2 (MAP2). It stimulates tubulin polymerization, promotes neurite extension, and provides neuroprotective effects against neurotoxic agents. This compound has significant applications in neurobiology research and studies focused on neuronal development and protection.
  4. Microtubule/Tubulin Inhibitor

    TN-16 is a potent microtubule polymerization inhibitor with an IC50 value ranging from 0.4 to 1.7 µM. It targets tubulin to disrupt microtubule dynamics, thereby affecting cellular processes such as mitosis and intracellular transport. TN-16 is useful in research applications exploring cancer biology and cellular function, making it an important tool for studying the role of microtubules in various diseases.
  5. Amino acid residues of Dolastatin 13

    N-Boc-dolaproine-methyl is an amino acid derivative derived from Dolastatin 10, a pentapeptide known for its role in inhibiting tubulin polymerization. This compound demonstrates significant anticancer activity by disrupting mitosis and cellular proliferation. It is valuable for research applications focused on cancer biology and the development of novel therapeutics targeting cytoskeletal dynamics.
  6. Microtubule/Tubulin Inhibitor

    Pironetin is an α/β unsaturated lactone derived from Streptomyces species that acts as a potent microtubule/tubulin inhibitor. By binding to α-tubulin, Pironetin effectively inhibits microtubule polymerization, leading to cell cycle arrest and exhibiting significant antitumor activity. This compound is valuable for research into cancer biology and the mechanisms of microtubule dynamics.
  7. Tubulin Destabilizer

    RGN6024 is a reversible small molecule tubulin destabilizer that effectively inhibits microtubule polymerization by targeting the colchicine binding pocket of β-tubulin. With a binding affinity of Kd = 6.7 μM as measured by surface plasmon resonance, RGN6024 induces G2/M phase arrest in glioblastoma cells and demonstrates efficacy in βIII-tubulin overexpressing cell models. Additionally, RGN6024 inhibits tumor growth in glioblastoma xenograft mouse models, making it a valuable tool for research into glioblastoma pathophysiology and therapeutic strategies.
  8. Microtubule/Tubulin Inhibitor

    Taccalonolide B is a microtubule stabilizer that targets tubulin, exhibiting notable antitumor activity. This compound demonstrates efficacy in vitro against cell lines with overexpression of P-glycoprotein (Pgp) and multidrug-resistance protein 7 (MRP7). Taccalonolide B effectively inhibits the growth of SK-OV-3 cells, yielding an IC50 value of 208 nM, making it a valuable tool for cancer research and drug resistance studies.
  9. Microtubule-targeting Agent

    ST-401 is a microtubule-targeting agent (MTA) that acts as an assembly inhibitor. By moderately and reversibly disrupting microtubule assembly, ST-401 induces mitotic delay and promotes cell death during interphase. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and studies focused on microtubule dynamics.
  10. Intermediate Reactant

    Monomethyl auristatin E intermediate-15 is a crucial intermediate in the synthesis of Monomethyl auristatin E (MMAE). MMAE functions as a microtubule and tubulin inhibitor, exhibiting significant anticancer activity. This compound is predominantly utilized as the cytotoxic component in antibody-drug conjugates (ADCs), thereby enhancing targeted cancer therapies. Its role in facilitating the production of MMAE makes it an important reagent for researchers focused on developing innovative cancer treatments.
  11. Microtubule Destabilizing Agent

    (S)-3-(4-(2-Chloro-5-iodobenzyl)phenoxy)tetrahydrofuran is a microtubule destabilizing agent. This compound demonstrates significant anticancer activity and can be employed in cancer research to elucidate mechanisms of tumor cell proliferation and apoptosis. Its halogenated structure enhances its interaction with microtubules, making it a valuable tool for studying cytoskeletal dynamics and evaluating potential therapeutic strategies.
  12. Microtubule/Tubulin Inhibitor

    OXi8007 is a water-soluble phosphate proagent of OXi8006, functioning as a microtubule/tubulin inhibitor. This compound effectively disrupts microtubule dynamics, leading to inhibition of cell proliferation and promotion of apoptotic processes. OXi8007 is widely utilized in cancer research and investigations focusing on the modulation of cytoskeletal structures.
  13. Anti-cancer Agent

    AMXI-5001 is a potent, orally active dual inhibitor of PARP1/2 and microtubule polymerization. This compound demonstrates selective antitumor cytotoxicity in various human cancer cell lines, exhibiting lower IC50 values compared to existing clinical PARP inhibitors. AMXI-5001 is capable of inducing complete regression of established tumors, including those of considerable size, making it a promising candidate for cancer research and therapeutic development.
  14. Tubulin Inhibitor

    Podophyllotoxone is a natural compound derived from the roots of Dysosma versipellis that acts as a tubulin inhibitor. It effectively disrupts tubulin polymerization, thereby interfering with the processes of cell division and inducing anti-cancer effects. This compound is utilized in cancer research to study its potential therapeutic applications in various malignancies.
  15. Microtubule Inhibitor

    Taccalonolide AJ is a microtubule stabilizing compound with significant antiproliferative properties. This semi-synthetic reagent demonstrates high potency against cancer cells, exhibiting an IC50 of 4.2 nM in HeLa cell lines. Its mechanism of action involves the stabilization of microtubules, making it a valuable tool for research in cancer biology and therapeutic development.
  16. Tubulin Inhibitor

    Phomopsin A is a cyclic hexapeptide mycotoxin that functions as a noncompetitive inhibitor of tubulin. It disrupts the binding of vincristine to tubulin, which is essential for microtubule dynamics. This compound is valuable in research exploring cell division and cancer biology, particularly in studies investigating the mechanistic action of tubulin-targeting agents.
  17. NQO1 Inhibitor

    Diminutol is a selective inhibitor of NADP-dependent quinone oxidoreductase (NQO1), an enzyme implicated in critical cellular processes such as microtubule morphogenesis and cell division. This compound has significant potential for research applications related to cancer biology and cellular dynamics, providing insights into the role of NQO1 in various pathological states. Its ability to modulate NQO1 activity makes it a valuable tool for studying the enzymatic pathways associated with oxidative stress and cellular proliferation.
  18. Tubulin Inhibitor

    Tubulin polymerization-IN-75 is a selective inhibitor of tubulin polymerization, demonstrating an IC50 of 30 μM. This compound significantly reduces the proliferation of cancer cell lines Huh7 and 293T, exhibiting IC50 values of 14.3 μM and 13.8 μM, respectively. It serves as a valuable tool for research aimed at investigating the mechanisms of cancer cell growth and the modulation of the cytoskeleton.
  19. β-tubulin Inhibitor

    Icafolin-methyl is an inhibitor of β-tubulin, targeting the colchicine binding site to prevent tubulin polymerization. This compound exhibits powerful post-emergence herbicidal activity against a range of weeds, including resistant strains such as ryegrass and darnel, making it suitable for application in both cool-season and warm-season cropping systems. Icafolin-methyl is valuable for research into herbicide mechanisms and the development of novel weed management strategies.
  20. Tubulin Inhibitor

    DJ101 is a potent tubulin inhibitor that binds to the colchicine site, effectively overcoming taxane resistance in cancer cells. This compound demonstrates significant biological activity by inhibiting tumor growth in melanoma and lung metastasis. DJ101 is a valuable reagent for research applications focused on prostate cancer and related pathways.
  21. Microtubule/Tubulin Inhibitor

    Curvulin is a microtubule/tubulin inhibitor that disrupts microtubule assembly, affecting cytoskeletal integrity and cellular dynamics. It also inhibits the expression of inducible nitric oxide synthase (iNOS), thereby modulating nitric oxide production. This compound is useful for research in cell biology, cancer studies, and investigations involving inflammation and nitric oxide signaling pathways.
  22. Centrosome Clustering Inhibitor

    CCCI-01 is a centrosome clustering inhibitor that selectively targets cancer cells. It disrupts centrosome clustering, presenting potential as a non-cross-resistant anti-cancer agent. This compound is useful for research applications aimed at understanding cell division anomalies and developing new therapeutic strategies for cancer treatment.
  23. Tubulin Inhibitor

    Tubulin Inhibitor 24 is a potent agent targeting tubulin polymerization. This compound effectively induces cell cycle arrest at the G2/M phase in a concentration-dependent manner, demonstrating significant antitumor activity. Its low toxicity profile makes it a valuable tool for cancer research applications.
  24. Paclitaxel Analogue

    Dihydrocephalomannine, a Paclitaxel analogue, exhibits lower cytotoxicity and diminished tubulin-binding affinity relative to its parent compound. This modified structure offers valuable insights into the mechanism of action of taxanes and their interactions with microtubules. As such, it serves as a useful tool in research applications aimed at understanding drug resistance and developing novel anti-cancer therapies.
  25. Tubulin Distabilizer

    Suprafenacine is a cell-permeable tubulin destabilizer that binds to microtubules at the colchicine-binding site, thereby inhibiting polymerization. By disrupting microtubule dynamics, Suprafenacine induces G2/M cell cycle arrest and promotes apoptosis, making it a valuable tool for cancer research. Its ability to interfere with microtubule formation provides insights into the mechanisms of tumor growth and potential therapeutic applications in oncology.
  26. Tubulin Modulator

    Isocephalomannine is a tubulin modulator that exhibits cytotoxic activity against cancer cells. This compound disrupts microtubule dynamics, leading to apoptotic cell death, particularly in breast cancer cells. Isocephalomannine is a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting microtubule stabilization and destabilization.
  27. Colchicine Analog

    3-Demethylthiocolchicine is a colchicine analog that exhibits broad-spectrum antitumor activity. It effectively blocks casein-induced amyloidosis and demonstrates microtubule binding while possessing anti-inflammatory properties. Notably, 3-Demethylthiocolchicine offers similar therapeutic effects as colchicine but with significantly reduced toxicity, making it a valuable tool for cancer research and potential therapeutic applications.
  28. Tubulin Inhibitor

    Tubulin polymerization-IN-47 is a potent inhibitor of tubulin polymerization, specifically targeting mitotic processes. This compound demonstrates significant inhibitory effects on neuroblastoma cancer cell proliferation, exhibiting IC50 values of 7 nM and 12 nM against the Chp-134 and Kelly cell lines, respectively. It is a valuable tool for research in cancer biology, particularly in the study of cell division and the mechanisms of tumor growth.
  29. Tubulin Polymerization Inhibitor

    Antiproliferative agent-14 is a potent tubulin polymerization inhibitor with an IC50 of 3.41 μM. This compound demonstrates significant antiproliferative activity, effectively disrupting cell cycle progression by arresting cells at the G2/M phase. It is a valuable tool for studying tumor biology and the mechanisms underlying cell division in cancer research.
  30. Tubulin/NEDDylation Inhibitor

    Tubulin/NEDDylation-IN-1 (compound C11) is a potent dual inhibitor targeting tubulin and NEDDylation, exhibiting an IC50 of 2.40 μM for tubulin. This compound effectively disrupts microtubule dynamics and inhibits the NEDDylation process, a crucial post-translational modification involving the attachment of the ubiquitin-like protein NEDD8 to target proteins. By forming hydrogen bonds with key residues in tubulin and the NEDD8 activating enzyme (NAE) through its methoxy and dithiocarbamate functionalities, Tubulin/NEDDylation-IN-1 demonstrates significant anti-proliferative activity and serves as a valuable tool for research investigating cellular proliferation and microtubule regulation.
  31. Tubulin Inhibitor

    Tubulin Inhibitor 6 targets tubulin polymerization, displaying potent inhibitory activity across various cancer cell lines. It demonstrates an IC50 of 0.87 μM for tubulin polymerization and effectively inhibits the growth of K562 cells with an IC50 of 840 nM. This compound is useful for research applications focused on elucidating mechanisms of cancer cell proliferation and treatment strategies.
  32. Ubulin Polymerization Inhibitor

    Tubulin polymerization-IN-51 is a potent tubulin polymerization inhibitor, exhibiting an IC50 value ranging from 2.55 to 17.89 μM in SK-Mel-28 cells. This compound effectively disrupts microtubule assembly, making it a valuable tool for cancer research. Its application in various experimental settings allows for the exploration of mechanisms underlying tumor cell proliferation and metastasis.
  33. Microtubule Stabilizer

    Microtubule Stabilizer-1 targets microtubule stabilization, enhancing the levels of acetylated α-tubulin (AcTub) in neuronal cells. This compound effectively prevents the loss of microtubules induced by Okadaic acid treatment, making it a valuable tool for investigating Alzheimer’s disease and related neurodegenerative tauopathies. Its ability to penetrate the blood-brain barrier further supports its application in neuroscience research.
  34. Microtubule/Tubulin Inhibitor

    OSIP-486823 is a novel tubulin inhibitor that disrupts microtubule dynamics. It demonstrates significant biological activity by affecting protein kinase G (PKG) pathways alongside its microtubule-interfering properties. This dual action positions OSIP-486823 as a valuable tool for studying cell division, cytoskeletal organization, and various signaling pathways in cancer research and other related fields.
  35. Tubulin Inhibitor

    Tesetaxel is a taxane tubulin inhibitor that demonstrates oral activity and effective brain penetration. It inhibits tubulin depolymerization with an IC50 of 0.44 μM, leading to a reduction in cancer cell proliferation. This compound exhibits potent antitumor effects, particularly against P-glycoprotein-positive cancer cells, making it valuable for research applications related to solid tumors, liver metastasis, and advanced breast cancer.
  36. Tubulin Targeting Agent

    PM534 is a tubulin-targeting agent that inhibits tubulin assembly with IC50 values ranging from 0.8 to 3.2 nM. By binding to the colchicine site of tubulin, PM534 disrupts microtubule dynamics, demonstrating significant antitumor activity. This compound is valuable for research applications in cancer biology, particularly in studies focused on cell division and microtubule-targeting therapies.
  37. Tubulin Polymerization Inhibitor

    S516 is a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. This active metabolite of CKD-516 exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to disrupt microtubule dynamics may provide insights into cell cycle regulation and potential therapeutic strategies against cancer.
  38. Tubulin Polymerisation Inhibitor

    Tubulin Inhibitor 27 (DYT-1) is a potent tubulin polymerisation inhibitor with an IC50 value of 25.6 μM. This compound exhibits significant anti-angiogenic and antitumor activities, making it valuable for research into cancer biology and potential therapeutic applications. Its ability to disrupt microtubule dynamics can aid investigations into cellular processes related to tumor growth and metastasis.
  39. Microtubule Inhibitor

    Microtubule Inhibitor 5 is a potent agent targeting microtubules, demonstrating significant cytotoxicity with an IC50 value of 154.5 nM in NCI-H460 cells. This compound exhibits favorable cell permeability, making it suitable for various research applications related to cancer biology and cell division. It provides valuable insights for studies investigating the mechanisms of microtubule disruption and its implications in tumor growth inhibition.
  40. Tubulin Inhibitor

    Tubulin Inhibitor 22 is a potent inhibitor of tubulin, demonstrating significant anti-angiogenic and anti-cancer properties. It effectively arrests the MGC-803 cell cycle at the G2/M phase, leading to a dose-dependent induction of Caspase-mediated apoptosis through mitochondrial dysfunction. This compound is valuable for research applications in cancer biology and the study of cell cycle regulation.
  41. Tubulin Inhibitor

    ABI-274 is a potent tubulin inhibitor that targets the colchicine binding site. This compound significantly enhances cancer cell apoptosis in vitro when used in combination with vemurafenib, exhibiting strong synergistic effects. In vivo studies demonstrate its efficacy in vemurafenib-resistant xenograft models in nude mice, making ABI-274 a critical tool for research on melanoma and potential therapeutic strategies in resistant cancer forms.
  42. Drug Isomer

    (R)-Taltobulin, also known as (R)-HTI-286, serves as a reference isomer utilized in drug development research. This compound is primarily studied for its effects on tubulin polymerization, which plays a critical role in cell division and cancer progression. Its applications include evaluating the pharmacological properties of microtubule-targeting agents and advancing cancer therapeutics.
  43. Anti-microtubular Agent

    Deacetoxyvinzolidine is a bis-indole derivative that functions as an anti-microtubular agent by disrupting microtubule assembly. It demonstrates a strong affinity for bovine purified brain tubulin, with a Kd of 3 μM, effectively inhibiting microtubule formation at concentrations as low as 10 nM. Its significant anti-tumoral properties make it a valuable tool for research, particularly in the investigation of leukemia and related malignancies.
  44. Negative Control

    Microtubule Destabilizing Agent-3 (negative control) is a reagent designed to serve as a negative control in studies investigating microtubule dynamics. While genuine microtubule destabilizing agents induce disruptions in the microtubule network and promote mitotic arrest, this negative control allows for the assessment of assay specificity. It is crucial for evaluating the role of microtubule destabilization in various cellular processes, including apoptosis and cell cycle regulation, without exerting direct biological effects.
  45. Antitumor Compound

    Vinzolidine is a semisynthetic derivative of catharanthus alkaloids that targets microtubulin polymerization to exert cytotoxic effects on tumor cells, inhibiting cell division. This antitumor compound is valuable in research for investigating synergistic effects with other chemotherapeutic agents or biologic therapies, as well as studying the tolerance and resistance of cancer cells to these treatments. Vinzolidine serves as a useful tool for exploring new strategies to overcome therapeutic challenges in cancer research.
  46. Anticancer Agent

    Anticancer agent 60, also known as compound 3h, primarily targets cancer cell proliferation. It exhibits significant antiproliferative activity against human HepG2 cells, with an IC50 value of 4.13 μM. Additionally, this compound demonstrates antitumor efficacy in a human HepG2 xenograft mouse model, making it a valuable tool for cancer research and therapeutic development.
  47. Tubulin Inhibitor

    Tubulin inhibitor 8 (Compound 33b) is a potent inhibitor of tubulin polymerization, demonstrating an IC50 value of 0.73 μM. This compound effectively inhibits the growth of K562 cancer cells, achieving an IC50 of 14 nM. Tubulin inhibitor 8 is valuable for studies in cancer research, particularly in evaluating mechanisms of action related to cytoskeletal dynamics and potential therapeutic interventions in tumor proliferation.
  48. Tubulin Inhibitor

    Tubulin Inhibitor 7 is a potent inhibitor of tubulin polymerization, targeting microtubule dynamics critical for cell division. With an IC50 of 0.52 μM, it effectively disrupts tubulin assembly, exhibiting significant anti-proliferative activity in various cancer cell lines. Notably, Tubulin Inhibitor 7 demonstrates an IC50 of 11 nM against K562 cells, making it a valuable tool for cancer research and studies focused on mitotic disruption.
  49. Tubulin Inhibitor

    Tubulin Inhibitor 29 is a potent inhibitor of tubulin assembly, exhibiting an IC50 value of 1.2 µM. This compound demonstrates significant antiproliferative activity, with an IC50 value of 7.5 µM against MCF-7 breast cancer cells. By binding to the colchicine site on tubulin, Tubulin Inhibitor 29 disrupts microtubule dynamics, making it a valuable tool for cancer research and studies focused on cell cycle regulation.
  50. Microtubule Inhibitor

    Cevipabulin fumarate dihydrate is a potent microtubule inhibitor targeting tubulin to disrupt microtubule dynamics. This orally administered antitumor compound demonstrates significant cytotoxic activity in human tumor cell lines, with an IC50 range of 18-40 nM. Cevipabulin is primarily used in cancer research to explore mechanisms of tumor cell proliferation and resistance, providing valuable insights for therapeutic development.

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