产品名称

英文名称：GF109203X

同义词

bisindolylmaleimide i、133052-90-1、GF 109203X、GF109203X、GF-109203X、Go 6850、Go-6850、3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione、3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione、Bisindolylm

产品性质

CAS编号：133052-90-1

分子式：C25H24N4O2

分子量：412.48

MDL号：MFCD00236428

PubChem编号：2396

英文别名：bisindolylmaleimide i|133052-90-1|GF 109203X|GF109203X|GF-109203X|Go 6850|Go-6850|3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione|3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione|Bisindolylm

规格或纯度：≥99%

英文名称：GF109203X

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 sμggests 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.Potent, selective PKC inhibitor (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC 50 = 360 nM). Potent 5-HT3 antagonist (K i = 29.5 nM).

应用：A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3

储存温度：2-8°C储存

运输条件：冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

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。 A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3GF109203X 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. A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3

IUPAC Name：3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione

INCHI：InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)

InChi Key：QMGUOJYZJKLOLH-UHFFFAOYSA-N

Canonical SMILES：CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

Isomeric SMILES：CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

WGK Germany：3

RTECS：UX9590000

PubChem CID：2396

CAS Registry No.：133052-90-1

ChEMBL Ligand：CHEMBL7463

Wikipedia：BIM-1

RCSB PDB Ligand：BI1

溶解性：Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 110 DMSOPBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.

敏感性：对热敏感

熔点：270 °C

象形图：

信号词：Warning

危险声明：H302 Harmful if swallowed

预防措施声明：P501,P264,P270,P330,P301+P317

产品包装