Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
Fmoc-L-Lys (Boc)-OH-13C6,15N2 is a 15N-labeled and 13C-labled Triclabendazole.
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM[1]. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research[1].
Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Zagotenemab (LY3303560) is a humanised anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research[1].
MMAF sodium (Monomethylauristatin F sodium) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF sodium is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel (HY-B0015). Anticancer activity[1][2].
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis[1].
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin[1].
Tubulin polymerization-IN-27 (compound 5j) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-27 can arrest cell cycle at G2/M phase and induce apoptosis[1].
Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].
Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase[1].
Glembatumumab vedotin (CDX-011) is an ADC (antibody-drug conjugates (ADCs)) comprising a fully human IgG2 monoclonal antibody (CR011) directed against glycoprotein NMB (GPNMB) and conjugated to the potent tubulinbinding cytotoxic agent MMAE via a protease-sensitive vc linker. Glembatumumab vedotin has potent anticancer effects[1].
Fmoc-MMAF-OMe is an anticancer agent and tubulin polymerization inhibitor with an Fmoc protecting group. The active ingredient of Fmoc-MMAF-OMe, MMAF (HY-15579), is the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs)[1].
Cephalomannine is a taxol derivative with antitumor, antiproliferative properties. IC50 value:Target: Cephalomannine is an active anti-cancer agent obtained from Taxus yunnanensis and has an antineoplastic effect on tumors found in mice. Cephalomannine is a chemotherapy drug that is given as a treatment for some types of cancer. Cephalomannine is most commonly used to treat non-small cell lung cancer.
Tubulin polymerization-IN-47 (Compound 4h) is a tubulin polymerization inhibitor and mitotic inhibitor. Tubulin polymerization-IN-47 inhibits neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell line[1].
Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
Polatuzumab vedotin is an antibody-drug conjugate targeting CD79b. It contains a humanized anti-CD79b IgG1 monoclonal antibody linked to monomethyl auristatin E (MMAE), a potent microtubule inhibitor. Polatuzumab vedotin has the potential for the research of Large B-cell lymphomas (LBCL)[1].
Tubulin polymerization-IN-18 (compound 8) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-18 has the potential for the research of breast cancers and chemoresistant colon cancers[1].
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties[1].Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities[1].
Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate (ADC).
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc[1]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro[2]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines[3].
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity[1].
Tubulysin IM-3 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity[1][2][3].
Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization[1].
Plocabulin (PM060184) is a novel tubulin-binding agent binding to αβ-tubulin dimer with nanomolar affinity, inhibits a panel of 23 tumor cell lines with GI50 of 20 pM-5 nM; inhibits angiogenesis by modulation of microtubule dynamics in endothelial cells; also shows antifungal activity virtually abolishing growth of the filamentous fungus Aspergillus nidulans.
Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis[1]. Deoxypodophyllotoxin induces cell autophagy and apoptosis[2]. Deoxypodophyllotoxin evokes increase of intracellular Ca2+ concentrations in DRG neurons[3].