tubulin

Tubulin Inhibitor 11 is a potent, orally active agent that inhibits tubulin by targeting the Colchicine binding site. It impedes tubulin polymerization, leading to mitotic blockade and apoptosis.

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.

MPI_5a is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM).

AC 7739 is a microtubule protein binding agent with anticancer and antitumor activity that inhibits advanced solid tumors and in situ transplanted tumors.

Vinorelbine ditartrate (KW-2307) is a natural alkaloid and an anti-mitotic agent. Vinorelbine ditartrate has anti-tumor activity, inhibiting cell proliferation and inducing apoptosis.

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.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

Verubulin (MPC 6827) is a potent microtubule blocker with cytotoxic and potentially anticancer activity that disrupts newly formed blood vessels in xenografts, and can be used to image microtubules (MTs) using positron emission tomography (PET).

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Cynaropicrin, a sesquiterpene lactone found in artichoke (Cynara scolymus), has anti-hepatitis C and trypanosome activity and inhibits NF-κB activation. Cynaropicrin disrupts microtubulin- and c-Myc-related signaling and induces parthanatos-type cell death in multiple myeloma.

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

T-900607 is a novel microtubule protein active agent that disrupts microtubule polymerization through a unique mechanism of action. t-900607 is cardiotoxic.

Cemadotin free base(LU103793 free base) is a novel anti-limiting peptide , an analog of Dolastatin 15, a naturally occurring cytotoxic peptide that blocks mitosis and inhibits microtubules (tubulin) with a Ki of 1 μM. Cemadotin is used in research against cancer.

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 24 is a potent compound that inhibits tubulin polymerization.

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

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 polymerization-IN-47 is a tubulin polymerization inhibitor and mitotic inhibitor with antitumor activity and inhibitory effects on neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell lines, respectively. Tubulin polymerization-IN-47 is a candidate compound for the treatment of hepatocellular carcinoma, colon cancer, lung cancer and breast cancer.

Tubulin inhibitor 7 is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines (tubulin polymerization (IC50: 0.52 μM), K562 cell growth (IC50: 11 nM)).

Tubulin inhibitor 1 is an inhibitor of tubulin, inhibits tubulin polymerization, with potent anti-tumor activity, induces cellular apoptosis causes and cellular mitotic arrest in the G2 M phase.

Compound 5L, also known as hTopo-II tubulin-IN-1, functions as an inhibitor of hTopo-II tubulin. It is effective in suppressing cell migration, making it valuable for use in anti-cancer research.

Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.

Tubulin polymerization-IN-69 (compound 6c) exhibits significant inhibition of microtubule assembly in vitro, with an inhibition rate of 78.3% and an IC50 value of 6.53 μM. It rapidly induces apoptosis and G2 M phase cell cycle arrest in MCF-7 cells.

Tubulin polymerization-IN-70 (compound Q19) is an effective inhibitor of tubulin polymerization. This compound exerts antiproliferative properties by targeting the colchicine binding site on tubulin, thereby inhibiting its polymerization. Tubulin polymerization-IN-70 also induces apoptosis and cell cycle arrest at the G2 M phase. Additionally, it triggers a decrease in mitochondrial membrane potential and elevates levels of reactive oxygen species (ROS). Moreover, Tubulin polymerization-IN-70 possesses anti-angiogenic and anticancer activities.