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GF109203X

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
G129390-1mg 133052-90-1 询价
G129390-50mg 133052-90-1 询价
G129390-10mg 133052-90-1 询价
产品介绍

  • 分子式 C25H24N4O2
  • 分子量412.48
  • Beilstein号
  • EC号
  • MDL号 MFCD00236428
  • PubChem编号

属性

溶解性 Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.
存贮条件 储存温度2-8℃

描述

应用 A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3
产品介绍 GF109203X是一种有效的PKC抑制剂,抑制PKCα, PKCβI, PKCβII和PKCγ,IC50分别为20 nM, 17 nM, 16nM和20 nM,作用于PKC比作用于EGFR, PDGFR和胰岛素受体选择性高3000倍以上。
备注 GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
生化机理 Bisindolylmaleimide I (GF 109203X) is a staurosporine inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. It inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases, as well as GSK-3.
别名 3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H-吡咯-2,5二酮;;双吲哚马来酰亚胺 I;Bisindolylmaleimide I;3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-Pyrrole-2,5-dione,

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途