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Todalam is a novel small molecule tubulin inhibitor with IC50 of 8.8 uM against HeLa cells, fully inhibits microtubule formation with IC50 of 48 uM, acting as a reversible microtubule-destabilizing agent in vitro and in cells.Todalam kills different type of mammalian cells, induces G2/M arrest, disrupts cellular microtubule networks, and can inhibit cell growth in a synergistic manner in combination with vinblastine.Todalam achieves its effect by locking α-tubulin in an inactive conformational state and by sequestering tubulin dimers.Todalam is the first-ever, fully rationally designed tubulin inhibitor with an original molecular mechanism of action.
FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.
SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer. SB-216 can be used for cancer research.
AM-5308 is a potent and selective KIF18A inhibitor with demonstrated antitumor activity in cell-based and animal models. Its ability to disrupt mitosis and induce cancer cell death makes it a promising candidate for further development as a cancer therapeutic.
Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals.
Docetaxal (10-Acetyl docetaxel; PNU-101383), an analog of Docetaxel, is a microtubule disassembly inhibitor, with antimitotic activity. Docetaxal has cytotoxicity for murine leukemic cells.
MAP4343 is the 3-methylether derivative of Pregnenolone. MAP4343 binds in vitro to microtubule-associated protein 2 (MAP2), stimulates the polymerization of tubulin, enhances the extension of neurites and protects neurons against neurotoxic agents.
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
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