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抑制剂/激动剂
囊泡 肿瘤
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细胞周期
其他抑制剂/激动剂 表观遗传学 TGF-beta/Smad 干细胞 外泌体 肿瘤表观遗传和基因调控 肿瘤干细胞 Wnt Notch
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转化生长因子-β SRPK PKC
/ Bisindolylmaleimide I

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

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.

Bisindolylmaleimide I 化学结构 CAS号：133052-90-1
Bisindolylmaleimide I 化学结构
CAS号：133052-90-1
Bisindolylmaleimide I 3D分子结构
CAS号：133052-90-1
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]}
批次查询： 批次纯度:

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更多 >
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 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

 		98%
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

 		PKA,EGFR 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

液体 -20°C:3-6个月-80°C:12个月

粉末 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

Tags: Bisindolylmaleimide I | 133052-90-1 | GF109203X | Go 6850 | Go6850 | Go 6850 | Go-6850 | PKC Inhibitor | Epigenetics | TGF-beta/Smad | Stem Cell/Wnt | PI3K/Akt/mTOR | PKC | GSK-3 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Bisindolylmaleimide I 纯度/质量文件 | Bisindolylmaleimide I 亚型比较 | 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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