In addition, low doses of synthetic drugs, such as the GSK-3 inhibitor IX (also known as BIO), an ATP-competitive inhibitor of GSK-3α/β, have found application in the pre-clinical evaluation of the beneficial effects of GSK-3 inhibition in the reduction of hepatic free fatty acid-depe...
We also review the current status of GSK-3 inhibitor development for innovative leukemia therapy.doi:10.1038/s41375-021-01243-zAlberto M. MartelliCamilla EvangelistiFrancesca PaganelliFrancesca ChiariniJames A. McCubreyLeukemia
9-ING-41 is a glycogen synthase kinase-3 inhibitor. 靶点活性 GSK-3β:0.71 μM (IC50) 体外活性 9-ING-41(2, 4 μM;48小时)能减少神经母细胞瘤细胞的活性并诱导凋亡[2]。9-ING-41(1, 2 μM;24小时)对淋巴瘤细胞具有强大的细胞周期阻断作用[2]。9-ING-41(0.1-1 μM)通过抑制GSK-3,从而降...
As a negative control, we used DMSO, the solvent in which the drugs were dissolved, and as a positive control we used lithium chloride, a well established GSK-3 inhibitor [41, 42]. When HeLa cells were treated with GSK-3 inhibitors for 24 hours, only SB-415286, AR-A014418, 1-Aza...
9-ING-41 is a small molecule potent selective GSK-3β inhibitor with antitumor activity. This study investigates 9-ING-41 in combination with carboplatin chemotherapy in patients with incurable, recurrent or metastatic salivary gland carcinomas (SGC). Patients with advanced SGC (including all histolo...
4.Ugolkov AV, et al. 9-ING-41, a small-molecule glycogen synthase kinase-3 inhibitor, is active in neuroblastoma. Anticancer Drugs. 2018 Sep;29(8):717-724. HB221117
GSK3182571 is a non-speci c kinase inhibitor[1]. 化学信息 分子量495.02 分子式C25H31ClN8O CAS No.2135595-04-7 密度1.298 g/cm3 (Predicted) 储存&溶解度 存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. ...
Figure 5. BIO Is a Selective GSK-3 Inhibitor in Cell Cultures (A) BIO inhibits the phosphorylation of β-catenin on GSK-3-specific sites. Cos-1 cells were untreated (mock) or exposed to 5 μM IO, BIO, MeBIO, or 20 mM LiCl for 24 hr. Proteins were then separated by SDS-PAGE fol...
CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Targets&IC50 GSK-3α:0.65 nM, GSK-3β:0.58 nM In vitro CHIR 98014 demonstrates significant efficacy in reducing hyperglycemia and enhancing glucose utilizat...
GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma. Targets&IC50 IKKε:469 nM, IKK2:790 nM, TBK1:93 nM ...