gpx 3

PROTAC GPX4 degrader-3, 作为一种高效的PROTAC GPX4降解剂,在HT1080细胞中展现出DC50(24 h)为0.019 μM和IC50为0.024 μM的优异活性.

GPX4-IN-3 (26a) 作为一种有效的谷胱甘肽过氧化物酶4 (GPX4) 抑制剂，其能选择性诱导铁死亡（ferroptosis）。在1 μM浓度下，该化合物能抑制GPX4活性达71.7%。

RC363 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It reduces 2,2-diphenyl-1-picrylhydrazyl radicals by approximately 40% in a cell-free assay when used at a concentration of 25 μM. RC363 prevents glutamate-induced toxicity in HT22 cultured hippocampal cells (IC50= 234.5 nM) but does not reduce oxidant levels in these cells. It increases the levels of glutathione peroxidase 1 (GPX1) and the activity of GPX in glutamate-challenged HT22 cells when used at a concentration of 3 μM. RC363 inhibits ferroptosis induced by the GPX4 inhibitor RSL3 in HT22 cells (IC50= 173.6 nM). 1.Bueno, D.C., Canto, R.F.S., de Souza, V., et al.New probucol analogues inhibit ferroptosis, improve mitochondrial parameters, and induce glutathione peroxidase in HT22 cellsMol. Neurobiol.57(8)3273-3290(2020)

Antitumor agent-77 对癌细胞的生长和迁移具有抑制作用，具有抗癌作用。Antitumor agent-77 能够抑制 GPx-4 和提高 COX2 引发铁下垂。Antitumor agent-77 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。

CCW 28-3 is a novel potent covalent BRD4 degrader, degrading BRD4 in a proteasome- and RNF4-dependent manner without inhibiting RNF4 autoubiquitination activity.

RC574 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It inhibits glutamate-induced cell death in HT22 cells (IC50= 276.2 nM) and mouse primary cortical neurons when used at a concentration of 3 μM. RC574 (3 μM) increases glutathione peroxidase 1 (GPX1) levels and GPX activity, as well as inhibits glutamate-induced mitochondrial superoxide anion production, in HT22 cells. It completely inhibits ferroptosis induced by the GPX4 inhibitor RSL3 in HT22 cells when used at concentrations ranging from 62.5 to 1,000 nM. 1.Bueno, D.C., Canto, R.F.S., de Souza, V., et al.New probucol analogues inhibit ferroptosis, improve mitochondrial parameters, and induce glutathione peroxidase in HT22 cellsMol. Neurobiol.57(8)3273-3290(2020)

3-Deoxyglucosone(3-Deoxy-D-glucosone) 是美拉德反应和多元醇反应的中间体途径合成。3-Deoxyglucosone 与蛋白质氨基快速反应形成晚期糖基化末端蛋白 (AGEs)。3-Deoxyglucosone 可使谷胱甘肽过氧化物酶失活，可与低葡萄糖协同作用以增强 GLP-1 分泌，可以作为糖尿病生物学检测的标志物。

Antitumor agent-78 能够抑制 GPx-4 和升高 COX2 ，进而导致铁下垂 (ferroptosis)。Antitumor agent-78 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，抑制肿瘤细胞上皮间质转化 (EMT) 过程。Antitumor agent-78 表现出抗肿瘤效果，并能够抑制癌细胞的生长和迁移。