g2 arrest

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2 M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar concentrations without damaging PLK1, a secondary target of AZD 1775.ZNL 02-096 induces degradation of Wee1 and accumulation of DNA damage in MOLT-4 cells in vitro, In vitro in MOLT-4 cells, ZNL 02-096 induced Wee1 degradation, accumulation of DNA damage, cell cycle arrest in G2 M phase and apoptosis.ZNL 02-096 showed anti-proliferative effects in 300 cancer cell lines.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2 M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2 M phase, underscoring its effectiveness as an antitumor agent.

Tubulin inhibitor 32 is an orally active novel microtubule inhibitor with antiproliferative and antitumor activity, inhibits microtubule polymerization, induces apoptosis and cell cycle arrest in G2 M phase.

(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor used as a clinical therapeutic agent against hepatoma.

Beta-Sitosterol (SKF 14463) has recently been shown to induce G2 M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K Akt signaling pathways. Beta-Sitosterol (SKF 14463) , a main dietary phytosterol found in plants, may have the potential for prevention and therapy for human cancer. Although the exact mechanism of action of Beta-Sitosterol (SKF 14463) is unknown, it may be related to cholesterol metabolism or anti-inflammatory effects (via interference with prostaglandin metabolism). Beta-Sitosterol (SKF 14463) induces apoptosis and activates key caspases in MDA-MB-231 human breast cancer cells.

Carbendazim (Mercarzole) is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities. Although the exact mechanism of action is unclear, carbendazim appears to binds to an unspecified site on tubulin and suppresses microtubule assembly dynamic. This results in cell cycle arrest at the G2 M phase and an induction of apoptosis.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

Sodium citrate (Natrocitral) is the sodium salt of citric acid.Citric acid trisodium induces apoptosis and cell cycle arrest at G2 M phase and S phase. Sodium citrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities.

Chlorahololide D is a natural lindane-type sesquiterpene dimer and selective potassium channel blocker that stimulates reactive oxygen species ROS levels to cause cell cycle arrest in the G2 phase, modulates Bcl-2 and Bax and FAK, thereby inhibiting MCF-7 cell growth and triggering apoptosis. Chlorahololide D inhibits tumor proliferation, migration and angiogenesis in in vivo experiments and has anti-breast cancer potential.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

Lexibulin (CYT-997)(CYT-997) is a potent tubulin polymerization inhibitor (IC50: 10-100 nM, in Y cell lines). Lexibulin blocks the formation of the mitotic spindle and leading to cell cycle arrest at the G2 M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death.

ABC1183 is a novel diaminothiazole that inhibits GSK3α, GSK3β and CDK9. ABC1183 inhibits the growth of a numerous cancer cell lines by decreasing cell survival by inducing G2 M arrest and through altering GSK3, glycogen synthetase, β-catenin phosphorylation and MCL1 expression,and is orally active.

GDC0575 monohydrochloride (ARRY575) is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2 M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.

1. Oxypeucedanin ((+-)-Oxypeucedanin) has novel anticancer effect, mediated via induction of G2-M cell cycle arrest and apoptosis in human prostate carcinoma DU145 cells. 2. Oxypeucedanin is a kind of open-channel blocker of the hKv1.5 channel and it prolongs the APD; therefore, it is an excellent candidate as an antiarrhythmic drug for atrial fibrillation.

MT189 (Antiproliferative agent-14) is a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2 M phases of the cell cycle.

IMS2186 is a reagent with activity of antichoroidal neovascularization (CNV). IMS2186 could arrest cancer cell cycle in G2 M phase, result in exerting anti-proliferation and anti-angiogenesis effects. IMS2186 reduces the amount of eye leakage and diseased cells with no intraocular toxicity.

Tubulin polymerization-IN-43 is an inhibitor of tubulin polymerisation.Tubulin polymerization-IN-43 has multiple effects, disrupting the cellular microtubule network by targeting the colchicine locus and promoting cell cycle arrest and apoptosis in leukaemia cells. Tubulin polymerisation-IN-43 has multiple effects, promoting leukaemia cell cycle arrest in G2 M phase and apoptosis by targeting Colchicine sites to disrupt the cellular microtubule network.

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.

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

Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2 M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

ER-076349 is a microtubule polymerization inhibitor that induces G2-M cell cycle arrest and disrupts mitotic spindles. This compound inhibits the growth of cancer cells and suppresses tumor growth in various human tumor xenograft mouse models. Additionally, ER-076349 is an analog of Halichondrin B.