Obatoclax Mesylate (GX15-070)

PubMed: 28382170      Theranostics

Western blotting showed that Obatoclax impacted cell cycle distribution through lowering cyclin D1 in K1 cells but in BCPAP cells, it impacted expression of p27 Kip1 rather than cyclin D1.

PubMed: 28035994      Int J Mol Sci

Cell line-dependent effect of obatoclax on cyclin D1 T286 phosphorylation. HCT116, HT-29, and LoVo cells were subject to 24 h-treatment with obatoclax (200 nM), followed by immunoblotting to evaluate the levels of threonine 286 (T286)-phosphorylated cyclin D1 (p-Cyclin D1) at indicated time points. α-Tubulin levels served as equal loading control;

PubMed: 28035994      Int J Mol Sci

Obatoclax inhibits GSK3β but activates p38 (MAPK), while barely affecting ERK1/2 activity in HT-29 cells. HT-29 cells were exposed to 200 nM of obatoclax for 24 h. The status of activation of GSK3β, ERK1/2, and p38(MAPK) at indicated time points was determined by immunoblotting for corresponding phosphorylation. Specifically, serine 9-phosphorylation of GSK3β (p-GSK3β) reveals inhibition of GSK3β activity, whereas dual phosphorylation at threonine 202/tyrosine 204 of ERK1/2 (p-ERK1/2) and threonine 180/tyrosine 182 of p38 MAPK (p-p38) indicate activation of ERK1/2 and p38(MAPK), respectively. α-Tubulin levels served as equal loading control;

PubMed: 28035994      Int J Mol Sci

Obatoclax inhibits colorectal cancer cell proliferation. Human colorectal carcinoma cell lines HCT116, HT-29, and LoVo cells were treated with obatoclax (0, 50, 100, 200 nM) for 24, 48, and 72 h. The numbers of cells at each time point were counted using a Neubauer chamber. Data were presented as the percentage relative to the drug-untreated control.

PubMed: 21368880      Cell Death Dis

H727 NSCLC cells are resistant to obatoclax. H727 and H1975 NSCLC cells were treated with obatoclax at the indicated doses for 48 (left) or 72 h (right), and the viability of cells determined by ViaLight assay. The EC50 values of cells at 48 h were; H1975 267 nM; H727 3.2 μM. The EC50 values of cells at 72 h were; H1975 66 nM; H727 621 nM. Data are expressed as mean±S.D.