Tubulin polymerization-IN-26 (compound 12h) can inhibit the polymerization of microtubulin by binding to the colchicine binding site of microtubulin with an IC50 value of 4.64 μM. Tubulin polymerization-IN-26 can induce apoptosis and inhibit cell metastasis or migration, and can be used as a potential compound for lung cancer research[1].
Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle[1].
VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects[1][2][3].
Neuroinflammatory-IN-3, a tubulin inhibitor, is an anti-neuroinflammatory agent. Neuroinflammatory-IN-3 is a potent antitumor agent that functions by the inhibition of tubulin polymerization[1][2].
LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer[1].
4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.IC50 Value: 0.31uM(EC5 0in HL60 cell, MTT assay, 48h); 0.37uM(EC50 in HepG2 cell, MTT assay, 48h) [1]Target: microtubulein vitro: 4-TMP-DMEP showed strong cytotoxicity activity against the above-mentioned five tumor cell lines. The EC50s of 4-TMP-DMEP against these tumor cell lines ranged from 0.24 to 0.11 μM, which were 0.29 to 3618 times lower than that of DMEP [1].in vivo: Treatment of animals with DMEP (until the end of the experiment), 30 min before TPA treatment, significantly reduced the tumor incidence, tumor volume and the conversion efficiency of papillomas to squamous cell carcinomas. The tumor formation and growth was also delayed by DMEP pre-treatment [2].
Rosabulin is a potent microtubule inhibitor, with anti-cancer activities.
FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research[1].
Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors[1].
Tubulysin I 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 I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule stabilizing agent. Dictyostatin also is a anti-cancer agent. Dictyostatin shows antiproliferative activity. Dictyostatin has the potential for the research of tauopathies[1][2][3].
Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM[1].
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
7-epi-Taxol is an active metabolite of taxol, with activity comparable to that of taxol against cell replication, promoting microtubule bundle formation and against microtubule depolymerization.
Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM[1][2].
Amiprofos methyl (BAY-NTN 6867) is a phosphoric amide herbicide. Amiprofos methyl is a specific and potent antimicrotubule agent. Amiprofos methyl directly poisons microtubule dynamics in plant cells[1].
Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity[1].
Paclitaxel D5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC[1].
KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity[1].
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases[1].
Vinblastine is a cytotoxic alkaloid used against various cancer types. Vinblastine inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.IC50 value: Target:BNC105 exhibited excellent potency against a panel of different cancer cell lines with IC50 <1 nM for DU145, Calu-6, MDA-MB-231 etc. The selectivity observed for BNC105 against activated over quiescent HUVECs was also observed in human aortic arterial endothelial cells (HAAECs). BNC105 also exhibited good potency toward the cisplatin resistant cell line A2780cis.
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM[1].
VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3].
Epothilone D is a potent microtubule stabilizer.
7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).