β-tubulin

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 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.

αβ-Tubulin-IN-1 is a potent, orally active inhibitor of αβ-Tubulin that blocks the cell cycle at the G2/M phase and induces apoptosis. It inhibits tumor cell migration and metastasis, exhibiting significant antitumor efficacy.

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).

Sabizabulin (ABI-231) is a potent, orally bioavailable α- and β-tubulin inhibitor that is active against melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells by targeting HPV E6 and E7 and is also being studied in prostate cancer.

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.

Ombrabulin hydrochloride is a synthetic, selective CA-4 phosphate ester or derivative of Ombrabulin to disrupt the tubulin cytoskeleton of endothelial cells and has antivascular effects. Ombrabulin is a tubulin polymerizing inhibitor, a member of the combretastatin A-4 compound class, which is a water-soluble tubulin depolymerizing tumor vascularizing compound.

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.

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

Tubulin inhibitor 24 is a potent compound that inhibits tubulin polymerization.

Triclabendazole (CGA89317) has been used in trials studying Parasitic Disease.

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

FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice. FC-116 induces apoptosis in colorectal cancer (CRC) cells and promotes protein degradation.

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.

Amphethinile, an anti-tubulin agent, has a Ka with tubulin of 1.3 μM.

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.

Mivobulin is an inhibitor of tubulin .

S-methyl DM1, a thiomethyl derivative of Maytansine, binds to tubulin (Kd of 0.93 μM) and inhibits microtubule polymerization.

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.

Tubulysin D is a tetrapeptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and displays potent antitumor activity.

SS28 inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase.

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM, demonstrating greater selectivity for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). It does not increase global histone H4 acetylation or reduce total intracellular HDAC activity but can induce tubulin acetylation[1][2].

Soblidotin (TZT-1027) (Auristatin PE) is an inhibitor of tubulin polymerization. It is also a novel synthetic Dolastatin 10 derivative.