CAS:133052-90-1Bisindolylmaleimide I

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Bisindolylmaleimide I Bisindolylmaleimide I Cat No. FB08457Cas No. 133052-90-1

Synonyms: GO 6850;Bisindolylmaleimide IGF109203X;GF 109203X

GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4243 mL
- 12.1217 mL
- 24.2434 mL
- 5 mM
- 0.4849 mL
- 2.4243 mL
- 4.8487 mL
- 10 mM
- 0.2424 mL
- 1.2122 mL
- 2.4243 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

133052-90-1

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C25H24N4O2

运输

蓝冰

分子量

412.48

别名

GO 6850;Bisindolylmaleimide IGF109203X;GF 109203X

溶解度

DMSO	80.0 mg/mL (193.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

靶点数据

生物活性

靶点 PKCβ2

IC50:16nM PKCβ1

IC50:17nM PKCα

IC50:20nM PKCγ

IC50:20nM
描述Protein kinase C (PKC) is a Ser/ Thr protein kinase whose activation is one of the earliest events in the cascade of signal transduction pathways leading to a variety of cellular responses such as secretion, gene expression, proliferation, and muscle contraction. Bisindolylmaleimide I, also called GF109203X, is a potent PKC inhibitor with IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively. GF109203X (20 nM) significantly increased the response to sciatic nerve stimulation in diabetic rats, producing a dilation not significantly different from controls. The administration of GF109203X was able to reverse the effects of hyperglycemia on NS1619 (10 µM)-mediated dilations. GF109203X significantly decreased mechanical withdrawal threshold (mean ± SEM: 7.75 ± 0.47 g vs 2.74 ± 0.43 g) and cold withdrawal latency (mean ± SEM: 7.66 ± 0.29 seconds vs 3.96 ± 0.79 seconds) in complete Freundʼs adjuvant (CFA)‐induced rheumatoid arthritis.
作用机制Bisindolylmaleimide I inhibits PKC activity exclusively via the ATP-binding site.
动物研究
剂量
Rat: 1 mg/kg^[3] (i.v.); 0.12 mg/kg (i.m.)

给药途径
i.v., i.m.

动物研究
剂量	Rat: 1 mg/kg^[3] (i.v.); 0.12 mg/kg (i.m.)
给药途径	i.v., i.m.

靶点	Description	IC50
PKCβ2		IC50:16nM
PKCβ1		IC50:17nM
PKCα		IC50:20nM
PKCγ		IC50:20nM