Bisindolylmaleimide VIII acetate | Ro 31-7549 acetate | PKC Inhibitor

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Bisindolylmaleimide VIII acetate {[allProObj[0].p_purity_real_show]}

货号：A1209442 同义名： Ro 31-7549 acetate; Bis VIII acetate

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2].

Bisindolylmaleimide VIII acetate 化学结构
CAS号：138516-31-1

Bisindolylmaleimide VIII acetate 3D分子结构
CAS号：138516-31-1

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Bisindolylmaleimide VIII acetate 纯度/质量文件产品仅供科研

货号：A1209442 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: 更多 >

肾上腺素能受体亚型比较
转化生长因子-β 亚型比较
PKC 亚型比较

产品名称	Adrenergic Receptor ↓ ↑	α-adrenergic receptor ↓ ↑	β-adrenergic receptor ↓ ↑	纯度
Ivabradine HCl	✔			98%
Maprotiline HCl	✔			98%
Cisatracurium besylate	✔			96%
Yohimbine HCI		✔		99+%
BMY 7378		++ α1D-adrenoceptor, pKi: 5.1 α2C-adrenoceptor, pKi: 6.54	+ β1-adrenoceptor, pIC50: 5.1	97%
Asenapine maleate		++++ α2B-adrenergic receptor, pKi: 8.9 α2A-adrenergic receptor, pKi: 8.9		97%
Piribedil		++ adrenoceptor α2C, pKi: 7.2 adrenoceptor α2A, pKi: 7.1		98%
Prazosin HCl		✔		95%
Silodosin		✔		98%
Phenoxybenzamine HCl		✔		98%
Naftopidil		+++ α1A-adrenergic receptor, Ki: 3.7 nM α1D-adrenergic receptor, Ki: 20 nM		98%
Naftopidil 2HCl		+ α1-adrenergic receptor, IC50: 0.2 μM		99%
Alfuzosin HCl		✔		98%
Terazosin HCl		✔		99%
Atipamezole		✔		95%
Phentolamine methanesulfonate salt		✔		99%
Doxazosin mesylate		✔		99%
Tolazoline HCl		✔		98%
Zenidolol HCl			++++ β2-adrenergic receptor, Ki: 0.7nM β1-adrenergic receptor, Ki: 611nM	98%
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	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 2HCl	++++ 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	+++ PKCβ2, IC50: 16 nM PKCβ1, IC50: 17 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	++ PKCβ2, IC50: 31 nM PKCβ1, IC50: 30 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	+++ PKCβ2, IC50: 14 nM PKCβ1, IC50: 24 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	++++ PKCβ2, IC50: 5.9 nM PKCβ1, IC50: 4.7 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 VIII acetate 生物活性

描述

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective inhibitor of protein kinase C (PKC). It exhibits an IC50 of 158 nM for rat brain PKC. Additionally, it shows IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively ^[1]. Bisindolylmaleimide VIII acetate enhances Fas-mediated apoptosis and suppresses T cell-mediated autoimmune diseases ^[2].
*该产品中的马来酰亚胺基团在碱性水溶液中会发生水解形成开环的马来酸酰胺衍生物，会影响生物学活性，例如无法和巯基形成共价硫醚键，影响和生物大分子的连接，建议现配现用，避免在水溶液中长期保存，可在中性或弱酸性水溶液中低温保存，反应时控制弱酸环境^[3][4]。

Bisindolylmaleimide VIII acetate 动物研究

Animal study

Bisindolylmaleimide VIII acetate (RO31-7549 acetate; 100 μg; i.p.; three doses every other day) in combination with TRA-8 results in near-complete tumor regression. Treatment with bisindolemaleimide VIII acetate alone does not cause significant tumor regression^[2].

Bisindolylmaleimide VIII acetate 参考文献

[1]Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7.

[2]Ohtsuka T, et al. Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways. J Biol Chem. 2002 Aug 9;277(32):29294-303.

Bisindolylmaleimide VIII acetate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.90mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

Bisindolylmaleimide VIII acetate 技术信息

CAS号	138516-31-1
分子式	C₂₆H₂₆N₄O₄
分子量	458.51
SMILES Code	O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC=C5)NC3=O.CC(O)=O
MDL No.	MFCD00909467

别名	Ro 31-7549 acetate; Bis VIII acetate; Bis VIII; 138516-31-1; Ro 31-7549; BIM VIII; Bisindolylmaleimide VIII (acetate); acetate; Bisindolylmaleimide VIII
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

溶解方案

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

Bisindolylmaleimide VIII acetate {[allProObj[0].p_purity_real_show]}

Bisindolylmaleimide VIII acetate 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 VIII acetate 质控信息

Bisindolylmaleimide VIII acetate 生物活性

Bisindolylmaleimide VIII acetate 动物研究

Bisindolylmaleimide VIII acetate 参考文献

Bisindolylmaleimide VIII acetate 实验方案

Bisindolylmaleimide VIII acetate 技术信息

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全球学术期刊中引用的产品

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Bisindolylmaleimide VIII acetate 技术信息

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总药量计算器

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