β-tubulin polymerization

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.

Ansamitocin p-3 (Maytansinol isobutyrate) is an inhibitor of microtubule with IC50 of 3.4 μM for tubulin polymerization.

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.

McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.It is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful agent for make antibody drug conjugate (ADC) for targeted drug delivery.

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.

Entasobulin is an inhibitor of β-tubulin polymerization. It has a potential anticancer activity.

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor targeting the colchicine-binding site. By inducing tubulin depolymerization, it inhibits the Wnt β-catenin pathway and deactivates AKT, possessing both anti-tumor and anti-vascular properties.

ABT-751 (E7010) hydrochloride is a novel sulfonyl anti-mitotic compound and a tubulin binder with high oral bioavailability. This agent binds to the colchicine site on β-tubulin, inhibiting the polymerization of tubulin which results in cell cycle arrest at the G2 M phase and induces apoptosis, effectively preventing cell division. Additionally, ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT MTOR signaling pathway. It exhibits significant inhibitory effects against various types of cancer cells, including lung, stomach, colon, and breast cancer.

PMMB276 is a powerful inhibitor of β-tubulin isotype III (Tubb3) polymerization that induces apoptosis, playing a crucial role in cancer research [1].

Tubulin polymerization-IN-53 (compound 4b) inhibits β-tubulin polymerization, arrests the cell cycle at the G2 M stage, and demonstrates antiproliferative efficacy against the MDA-MB-231 cell line, with an IC50 value of 3.24 μM [1].

VEGFR-2-IN-22 (Compound 25) is an inhibitor of VEGFR-2 and β-tubulin polymerization, with an IC50 of 19.82 nM for VEGFR-2, and is capable of inducing apoptosis.

Tubulin Polymerization-IN-2 is a powerful anticancer agent that targets β-tubulin, exhibiting an IC 50 of 0.92 μM. It demonstrates promising efficacy against a range of cancer cell lines including leukemia, non-small cell lung, renal, prostate, and breast cancers [1].

Icafolin-methyl is a plant-specific herbicide that acts as an inhibitor of tubulin polymerization. In plants, it metabolizes into the carboxylic acid icafolin, potentially inhibiting plant tubulin polymerization by binding to β-tubulin.

Pironetin binds to α-tubulin and is an effective inhibitor of microtubule polymerization. It also has cell cycle arrest and antitumor activity. Pironetin is an α β unsaturated lactone isolated from Streptomyces species.

Batabulin (T138067) is an antitumor compound that binds covalently and selectively to a subset of the β-tubulin isotypes, disrupting microtubule polymerization. This disruption affects cell morphology, induces cell-cycle arrest, and ultimately leads to apoptotic cell death.

Valecobulin is a potent β-tubulin polymerization inhibitor. Valecobulin is a valine prodrug of (S516) and an avascular disrupting compound.

Batabulin sodium (T138067 sodium) is an antitumor agent that covalently and selectively modifies β-tubulin isotypes, disrupting microtubule polymerization, affecting cell morphology, leading to cell-cycle arrest, and ultimately inducing apoptotic cell death [1].

MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein expression in the TGF-β SMAD pathway. This compound effectively reduces cell proliferation and migration while inducing apoptosis in both in vivo and in vitro settings [1].

Valecobulin hydrochloride (CKD-516 hydrochloride) is the valine prodrug and vasoblocker of S516. Valecobulin hydrochloride (CKD-516 hydrochloride) has a potent inhibitory effect on β-tubulin polymerization and has significant anti-tumor activity against solid tumors in mice and humans.