anti-mitotic

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest.

DMU-212 is a methylated derivative of resveratrol with antimitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It induces mitotic arrest, apoptosis, and activation of ERK1/2 protein and has oral activity[1][2]. DMU-212 (0.3125-40 μM) inhibits the growth of human melanoma cells (A375, MeWo, Bro, M5)[1]. At concentrations of 30-50 μM over 24 hours, it upregulates cell cycle inhibitors, induces apoptosis, and activates ERK in A375 cells[1]. DMU-212 also induces G2/M arrest and apoptosis in cancer cells[1]. In a xenograft model of human ovarian cancer with six-week-old SCID female mice (20-24 g), DMU-212 (50 mg/kg, administered orally three times a week for 14 days) inhibits tumor growth[2]. [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1/2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.

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.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

CHM-1 is an inducer of apoptosis, and displays potent antitumor ability in human hepatocellular carcinoma by activation of Cdc2 kinase activity. CHM-1 inhibits tubulin polymerization in vitro and in vivo.

Estramustine phosphate sodium (Ro 21-8837/001) is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) inhibits tubulin polymerization (IC50 = 4 μM) and has anti-mitotic effects.

Maleuric acid (N-Carbamoylmaleamic acid) is anti-mitotic and can be used in biological research in conjunction with radioautography.Maleuric acid is used to improve the growth and fertility of plants and animals as well as to treat whey acid deficiency.

Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antidiarrhoeic, antilipolytic, antispasmodic, and anti-tumor properties. Zingerone (Gingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways, acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

PAIB-SOs-12 is an anti-mitotic compound that shows anti-proliferative activity at low concentrations and induces cytoskeletal damage in MCF7 cells.

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM.

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.

SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), consisting of the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) linked via the cleavable linker SC-VC-PAB[1].

SuO-Val-Cit-PAB-MMAE is an ADC (antibody-drug conjugate) linker composed of the anti-mitotic monomethyl auristatin E (MMAE, a tubulin inhibitor) linked via the SuO-Val-Cit-PAB peptide.

DNA crosslinker 6 (compound 1) is an anti-mitotic agent known for its strong binding affinity to AT-DNA and inhibition of AT-hook 1 binding to DNA (IC50=0.03 µM). Additionally, it exhibits anti-protozoal activity, effectively inhibiting T. brucei with an EC50 of 0.83 µM.

Tubulysin Aintermediate-1 is an intermediate in the synthesis of the cytotoxic peptide Tubulysin A. Tubulysin A (TubA) acts as an antibiotic (antibiotic), anti-microtubule toxins (anti-microtubule toxins), and apoptosis (apoptosis) inducer, which can be isolated from myxobacteria. It exhibits anti-angiogenic, anti-microtubule, anti-mitotic, and anti-proliferative properties, effectively blocking cells in the G2/M phase, inhibiting tubulin polymerization, and inducing depolymerization of isolated microtubules. Tubulysin A serves as an ADC Cytotoxin (ADC Cytotoxin) in the synthesis of ADCs.

TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity.

Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for antibody-drug conjugates (ADCs), incorporating the tubulin inhibitor monomethyl auristatin E (MMAE) and linked via the cleavable Azido-PEG4-Val-Cit-PAB-OH.

KIF18A-IN-1 is a potent inhibitor of the mitotic kinesin KIF18A. This compound demonstrates significant anti-tumor properties.

Tasisulam is an anti-cancer compound that induces apoptosis through the intrinsic pathway, leading to the release of cytochrome c and caspase-dependent cell death. Additionally, tasisulam inhibits mitotic progression and triggers vascular normalization.

KIF18A-IN-4 is a moderately potent, non-competitive KIF18A inhibitor of ATP and microtubule with an IC50 of 6.16 μM. It selectively acts on many mitotic kinesins and kinases, without directly affecting microtubule protein assembly, and shows anti-tumour effects.

Vinorelbine ditartrate (KW-2307) is a natural alkaloid and an anti-mitotic agent. Vinorelbine ditartrate has anti-tumor activity, inhibiting cell proliferation and inducing apoptosis.