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.

GSK-1 is an ATP-competitive inhibitor of the mitotic kinesin KSP with HCT116 cell IC50 of 36 nM; induces monopolar spindle formation in SKOV3 cells, and shows markedly greater potency (IC50 of 0.5 nM) in the ispinesib-resistant HCT116-D130V cell line.

C67399 is a small molecule that blocks the integrin β1 binding site of TLN1, reduces the malignant behaviours of TNBC in vitro (MDA-MB-231 cell, IC50=2.0 uM).C67399 treatment significantly reduced the viability of BT549 cells.C67399 (2 uM) significantly reduced the expression of integrin β1, AKT, FAK, and phosphorylated FAK in MDA-MB-231 cells, while did not affect the expression of integrin β3.C67399 inhibited the binding of TLN1 to integrin β1 in MDA-MB-231 cells.C67399 (1.75 mg/kg) inhibited tumour growth and metastasis of MDA-MB-231 cells in mice, without causing obvious structural toxic changes.

Azo-EMD is a cell permeable, photoswitchable compound that inhibits mitotic kinesin Eg5 more potently in its light-induced cis form, used for optical control mitosis.Under UV light conditions, HeLa cells undergo mitotic arrest, as evidenced by the formation of a monopolar spindle.

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.

Alicaforsen is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.

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.

TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells.

Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis. CME: Clathrin mediated endocytosis

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.

Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels.

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.

αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .

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.

MiTMAB is a selective dynamin inhibitor that targets the dynamin-phospholipid interaction. MiTMAB inhibits dynamin GTPase activity with a Ki of 940 nM.

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

CK-666 is an inhibitor of the actin-related protein 2/3 (Arp2/3) complex with IC50 of 17 μM and 5 μM for BtArp2/3 complex and SpArp2/3 complex, respectively.

α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.

Vinflunine Tartrat is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.

MT-134 is a SkMII-specific inhibitor and has excellent exposure in muscles.

Dolastatinol is a synthetic analog of dolastatin 10 and low nanomolar inhibitor of tubulin polymerization.