AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1].
Tubulin polymerization-IN-38 a Tubulysin (HY-128914) analogue, is a potent anticancer agent. Tubulin polymerization-IN-38 inhibits tubulin polymerisation and thereby inducing apoptosis. Tubulin polymerization-IN-38 has cytotoxicity against cancer cells[1].
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].
Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM.
Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].
Oryzalin is a dinitroaniline herbicide, binding to plant tubulin and inhibits microtubule (MT) polymerization in vitro. Oryzalin depolymerizes MTs and prevented the polymerization of new MTs at all stages of the mitotic cycle[1].
Tubulin polymerization-IN-43 (compound 15h) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-43 disrupts cellular microtubule networks by targeting the Colchicine (HY-16569) site, and promots cell cycle arrest of leukemia cells at G2/M phase and cell apoptosis, as well as inhibiting angiogenesis[1].
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis[1].
Docetaxel Trihydrate is a semi-synthetic taxane analogue, acts as a microtubule stabilizer.
Tubulysin F 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 F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
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].
Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types[1].
Tubulysin M 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 M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].
Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM[1].
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells[1].
S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell Apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].
ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
D8-MMAE is a deuterated labeled MMAE, a potent mitotic inhibitor.
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.
TN-16 is a potent inhibitor of microtubule polymerization with IC50 of 0.4-1.7 µM[1].
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].
Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis[1].
Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more potent drug than Monomethyl auristatin E (MMAE), but is charged and relatively membrane-impermeable, is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.Target:MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity [1].
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].