Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel. Anticancer activity.

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.

SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs.

Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo.

HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.

IQTub4P is a potent microtubule (MT) inhibitor. IQTub4P has the cytotoxicity in in HeLa cells, with EC50 of 170 nM. IQTub4P inhibits microtubule structure and function. IQTub4P is well-tolerated in vivo.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD)  brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe.

isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities.

THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD)  brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe.

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.

PST-3 (Microtubule inhibitor PST-3) is a novel microtubule inhibitor exhibited broad-spectrum cellular cytotoxicity and in vivo potency with high safety.PST-3 inhibits different cancer cell with high safety (BT549 IC50=15 uM, MDA-MB-468 IC50=16 uM), inhibits human breast cancer cell clonogenic growth with IC50 values rang from 3 uM to 25 uM (MDA-MB-231 cell IC50=11.43 uM).PST-3 binds to the colchicine binding site on microtubule, induces morphological changes, disrupts the structure of microtubule in cells and inhibits tubulin polymerization, arrests BT549 and MDA-MB-468 cells in G2/M phase.PST-3 shows preferential growth inhibition in triple-negative breast cancer xenografts growth without neurotoxicity in vivo.

PCH-1 is a potent antitumor agent that disrupts microtubule assembly, leading to cancer cell death, interacts vinblastine binding site on tubulin; PCH-1 exhibits the strongest cytotoxic activity through interaction with tubulin, leading to cell cycle arrest and induction of apoptosis. PCH-1 efficiently inhibits the growth of NSCLC cancer cell lines at micromolar concentrations (A-549 IC50=4.32 uM, H226 IC50=4.69 uM), and non-toxic to normal cells.

Microtubule inhibitor PP-13 is a novel microtubule-destabilizing agent, directly inhibits microtubule assembly by targeting the colchicine-binding site in β-tubulin.PP-13 inhibits the growth of a wide range of cancer cell types, including targeted therapy-resistant and multidrug-resistant (MDR) cell lines (IC50=76-255 nM).PP-13 overcomes the multidrug-resistant (MDR) phenotype in cancer cells, induces mitotic blockade in cancer cells, interferes with both mitotic microtubule organization and spindle pole integrity.PP-13 induces cell prometaphase arrest then asymmetric division or direct apoptotic death.PP-13 reduces tumour growth and metastasis invasion in vivo.

IMB5476 (IMB 5476) is a nitrobenzoate microtubule inhibitor, exerts broad-spectrum cytotoxicity against various human tumor cell lines (NCI-H460, IC50=144 nM).IMB5476 inhibits purified tubulin polymerization in vitro, binds to tubulin at the colchicine pocket.IMB5476 induced cell death by mitotic catastrophe and apoptosis, disrupted microtubule networks in cells and arrested cell cycle at G2/M phase.IMB5476 is a poor substrate of P-glycoprotein and exhibited potent cytotoxicity against drug-resistant tumor cells.IMB5476 inhibited angiogenesis in vitro, also inhibited the growth of drug-resistant KBV200 xenografts in mice.

A small molecule that inhibits tubulin polymerization.

Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.

AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors.

Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity.

2-Methoxyestradiol-13C6 (2-ME2-13C6) is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.

OXi8007 is a water-soluble phosphate prodrug of OXi8006, a tubulin-binding compound.

(S)-AM-5308 (compound 7-13) is a potent kinesin KIF18A inhibitor with an IC50 of 46 nM for KIF18A ATPase. (S)-AM-5308 has the potential for cancer research.

VERU-111 (Sabizabulin) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities. Sabizabulin is a novel oral agent with both anti-viral and anti-inflammatory activities.Sabizabulin is a cytoskeleton disruptor which by causing microtubule depolymerization has both anti-viral and anti-inflammatory activity and could be effective against the SARS-CoV-2 virus by disrupting its intracellular transport along the microtubules. Microtubule trafficking is critical for viruses to be transported, replicated, assembled, and released from the cell. In addition, microtubule depolymerization drugs that target the “colchicine binding site” of microtubules, like sabizabulin, also have strong anti-inflammatory effects, including the potential to treat the cytokine release syndrome (cytokine storm) and septic shock induced by the SARS-CoV-2 viral infection that is associated with high COVID-19 mortality rates.

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.

Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM.

Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer.

DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2'-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.

Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.

Eribulin is an anticancer drug marketed by Eisai Co. under the trade name Halaven. Eribulin is also known as E7389 and ER-086526, and also carries the US NCI designation NSC-707389. It is used to treat certain patients with breast cancer and liposarcoma.

PF-06380101 D8 (Aur0101 D8) is a deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue.