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℃ |
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, |
双吲哚马来酰亚胺I
GF109203X (订货以英文为准)
编号:G129390
CAS号:133052-90-1
分子式:C25H24N4O2
分子量:412.48
产品名称 | GF109203X |
中文名称 | 双吲哚马来酰亚胺I |
CAS号 | 133052-90-1 |
MDL编码 | MFCD00236428 |
分子式(M.F.) | C25H24N4O2 |
分子量(M.W.) | 412.48 |
储存条件 | 2-8°C储存 |
标识符号 | https://www.aladdin-e.com/images/ghs/ghs07.jpg |
信号词 | Warning |
危害声明 | H302 |
个人防护设备 | dust mask type N95 (US), Eyeshields, Gloves |
WGK德国 | 3 |
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