microtubule/tubulin

Vinorelbine ditartrate (KW-2307), a semi-synthetic vinca alkaloid, interacts with tubulin resulting in mitosis inhibition.

Mertansine (DM1) refers to the thiol-containing maytansinoid, DM1 (N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Valecobulin hydrochloride (CKD-516 hydrochloride) is a potent inhibitor of β-tubulin polymerization. Valecobulin hydrochloride is a valine prodrug and a vascular disrupting agent.

Cephalomannine (Baccatin III) is a taxol derivative obtained from Taxus yunnanensis with antitumor activity.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

Combretastatin A4 (CA4) is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM).

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

10-Deacetyltaxol (10-DAT) is extracted from Taxus brevifolia barks.

Vincristine sulfate (Leurocristine sulfate) binds irreversibly to microtubules and spindle proteins in S phase and interferes the formation of the mitotic spindle.

Tubulin polymerization-IN-43 is an inhibitor of tubulin polymerisation.Tubulin polymerization-IN-43 has multiple effects, disrupting the cellular microtubule network by targeting the colchicine locus and promoting cell cycle arrest and apoptosis in leukaemia cells. Tubulin polymerisation-IN-43 has multiple effects, promoting leukaemia cell cycle arrest in G2/M phase and apoptosis by targeting Colchicine sites to disrupt the cellular microtubule network.

Tubulin inhibitor 24 is a potent inhibitor that can inhibit tubulin polymerization.

Tubulin inhibitor 32 is an orally active novel microtubule inhibitor with antiproliferative and antitumor activity, inhibits microtubule polymerization, induces apoptosis and cell cycle arrest in G2/M phase.

Tubulin inhibitor 35 (Tubulin IN 35) is a potent dual inhibitor of topoisomerase I and microtubule protein polymerization with antitumor activity, inhibits migration and invasion of MGC-803 and RKO cell lines, interrupts the cell cycle and induces apoptosis.

MKC-1 (Ro-31-7453) is an orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

Cevipabulin (TTI-237) is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) inhibits tubulin polymerization (IC50 = 4 μM) and has anti-mitotic effects.

Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.

Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

Ixabepilone (Azaepothilone B) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) is a drug-linker conjugate for ADC. Mc-MMAE is a maleimidocaproyl-conjugated monomethyl auristatin E, which is a potent tubulin inhibitor.

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

Monomethyl auristatin E (MMAE) (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity.

Nocodazole (Oncodazole) is a reversible inhibitor of microtubule polymerization and an inhibitor of Bcr-Abl. Nocodazole has antitumor activity, blocks the cell cycle and induces apoptosis.

Colchicine (Colcin) is a natural product that is an inhibitor of microtubule polymerization (IC50=3 nM) and blocks microtubule polymerization by binding to microtubule proteins. Colchicine can be used in the treatment of ventilation and rheumatic diseases.

Map4343 is a 3-methyl ether derivative of pregnenolone. Map4343 binds to microtubule associated protein 2 (MAP2) in vitro and stimulates tubulin polymerization, resulting in enhanced neurite extension and protection of neurons from neurotoxic agents.

Verubulin hydrochloride (MPC-6827 hydrochloride) is an agent of blood brain barrier permeable microtubule-disrupting, with potent and broad-spectrum cytotoxic activities,with potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models.

Rhizoxin is an antitumor drug isolated from the fungus Rhizopus chinensis. It is a macrocyclic lactone compound that binds to tubulin and inhibits microtubule assembly.

ELR510444 (LR510444) is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.

BRD9876 is a selective inhibitor of MM1S growth.

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins .

ALB-109564 dihydrochloride is a semi-synthetic derivative of the vinka alkaloid vinblastine with potential antineoplastic activity, a microtubule protein inhibitor and antineoplastic compound. It binds to tubulin monomers and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the G2/M phase of the cell cycle.

Ansamitocin P 3' (Maytansinol butyrate) is an antibody-drug conjugate cytotoxin with antitumor activity.

BNC105 is a tubulin polymerization inhibitor. It has potent antiproliferative and tumor vascular disrupting properties.

Myoseverin, an inducer of the reversible fission of multinucleated myotubes into mononucleated fragments, affecting the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with

KIF18A-IN-2 is an inhibitor of mitotic kinesin Kif18A with IC50 of 28 nM and can be used in studies about chromosomal instability-associated vulnerabilities.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

Curvulin is the active metabolite isolated from Paraphoma sp. VIZR 1.46. Curvularin inhibits iNOS expression and microtubule assembly.

Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.

Tubulin polymerization-IN-29 is a potent inhibitor of microtubule protein polymerization and shows potent anti-proliferative effects.Tubulin polymerization-IN-29 induces cell cycle arrest in HeLa cells at G2/M phase.

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibiting tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].

Compound 3l, a paclitaxel derivative known as Microtubule Stabilizing Agent-1, effectively enhances tubulin polymerization and demonstrates antitumor efficacy [1].

KGP591, a tubulin polymerization inhibitor with an IC50 of 0.57 µM, effectively induces G2/M arrest, inhibits cell migration, and disrupts microtubule structure and cell morphology in MDA-MB-231 cells. Additionally, it demonstrates antitumor activity in an orthotopic kidney cancer model (RENCA) [1].

Tubulin polymerization-IN-46 (compound 9q) is a microtubule/tubulin inhibitor that impedes tubulin polymerization, induces apoptosis, and arrests MCF-7 breast cancer cells in the G2/M phase, exhibiting potent anti-proliferative activity with an IC50 of 10 nM [1].

Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule destabilizer with potential tumor-selective as well as anti-angiogenic and vascular-destructive properties [1].

Entasobulin is an inhibitor of β-tubulin polymerization. It has a potential anticancer activity.