Bisindolylmaleimide I | Go 6850 | PKC Inhibitor | AmBeed-信号通路专用抑制剂

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双吲哚马来酰亚胺I /Bisindolylmaleimide I {[allProObj[0].p_purity_real_show]}

货号：A439059 同义名： Go 6850;GF109203X

Bisindolylmaleimide I是一种强效 PKC 抑制剂，在细胞外试验中对 PKCα、PKCβI、PKCβII 和 PKCγ 的 IC50 分别为 20 nM、17 nM、16 nM 和 20 nM，显示出比 EGFR、PDGFR 和胰岛素受体高达 3000 倍的选择性。

Bisindolylmaleimide I 化学结构
CAS号：133052-90-1

Bisindolylmaleimide I 3D分子结构
CAS号：133052-90-1

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Bisindolylmaleimide I 纯度/质量文件产品仅供科研

货号：A439059 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

转化生长因子-β 亚型比较
PKC 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		99%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									EGFR,PKA	95%
Dequalinium Chloride											99%+
Quercetin	✔									Sirtuin,Src	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 μM			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Bisindolylmaleimide I 生物活性

靶点	PKCβ PKCβ1, IC50:17 nM PKCβ2, IC50:16 nM PKCγ PKCγ, IC50:20 nM PKCα PKCα, IC50:20 nM
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^[3]. 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^[4]. 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^[5].
作用机制	Bisindolylmaleimide I inhibits PKC activity exclusively via the ATP-binding site.

Bisindolylmaleimide I 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay		Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells	19540764
mouse RAW264.7 cells		Function assay	24 h	Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay, IC50=0.19055 μM	17485504

Bisindolylmaleimide I 动物研究

Dose	Rat: 1 mg/kg^[3] (i.v.); 0.12 mg/kg (i.m.)
Administration	i.v., i.m.

Bisindolylmaleimide I 参考文献

[1]Vetri F, Qi M, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.

[2]Toullec D, Pianetti P, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81.

[3]Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. PMID: 1874734.

[4]Vetri F, Qi M, Xu H, Oberholzer J, Paisansathan C. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54. doi: 10.1016/j.brainres.2016.11.012. Epub 2016 Nov 16. PMID: 27865779; PMCID: PMC5195876.

[5]Bai Q, Shao J, Cao J, Ren X, Cai W, Su S, George S, Tan Z, Zang W, Dong T. Protein kinase C-α upregulates sodium channel Nav1.9 in nociceptive dorsal root ganglion neurons in an inflammatory arthritis pain model of rat. J Cell Biochem. 2020 Jan;121(1):768-778. doi: 10.1002/jcb.29322. Epub 2019 Aug 5. PMID: 31385361.

Bisindolylmaleimide I 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL

Bisindolylmaleimide I 技术信息

CAS号	133052-90-1
分子式	C₂₅H₂₄N₄O₂
分子量	412.484

别名	Go 6850;GF109203X;GO6850. BIMI.;bisindolylmaleimide;Gö 6850;BIM I
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 30 mg/mL(72.73 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

双吲哚马来酰亚胺I /Bisindolylmaleimide I {[allProObj[0].p_purity_real_show]}

Bisindolylmaleimide I 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Bisindolylmaleimide I 质控信息

Bisindolylmaleimide I 生物活性

Bisindolylmaleimide I 细胞研究

Bisindolylmaleimide I 动物研究

Bisindolylmaleimide I 参考文献

Bisindolylmaleimide I 实验方案

Bisindolylmaleimide I 技术信息

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PKCβ	PKCβ1, IC50:17 nM PKCβ2, IC50:16 nM
PKCγ	PKCγ, IC50:20 nM
PKCα	PKCα, IC50:20 nM

双吲哚马来酰亚胺I /Bisindolylmaleimide I {[allProObj[0].p_purity_real_show]}

Bisindolylmaleimide I 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Bisindolylmaleimide I 质控信息

Bisindolylmaleimide I 生物活性

Bisindolylmaleimide I 细胞研究

Bisindolylmaleimide I 动物研究

Bisindolylmaleimide I 参考文献

Bisindolylmaleimide I 实验方案

Bisindolylmaleimide I 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Bisindolylmaleimide I 纯度/质量文件产品仅供科研