Bisindolylmaleimide X HCl | BIM-X hydrochloride | PKC/CDK2 Inhibitor

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Bisindolylmaleimide X HCl {[allProObj[0].p_purity_real_show]}

货号：A1159144 同义名： BIM-X hydrochloride;Ro31-8425 hydrochloride

Bisindolylmaleimide xHCl is a potent protein kinase C (PKC) inhibitor.

Bisindolylmaleimide X HCl 化学结构
CAS号：145317-11-9

Bisindolylmaleimide X HCl 3D分子结构
CAS号：145317-11-9

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Bisindolylmaleimide X HCl 纯度/质量文件产品仅供科研

货号：A1159144 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

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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		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 X HCl 生物活性

描述

The protein kinase C (PKC) family of isozymes are involved in various cellular physiological processes, including cell proliferation, differentiation, apoptosis, glycogenolysis, and ion channel regulation. Bisindolylmaleimide X HCl (BisX) is a PKC inhibitor with an IC50 value of 15nM against rat brain PKC. It also inhibits PKCα, βI, βII, γ, and ε with IC50 values of 8, 8, 14, 13, and 39nM, respectively^[1]. Moreover, BisX was shown as a potent antagonist of cyclin-dependent kinase 2 with an IC50 value of 200nM^[2]. In HEK 293 cells, a 60-min pre-incubation with BisX (60nM) inhibited PMA-induced Ca²⁺ entry without affecting the basal calcium level. The pre-exposure of BisX also significantly prolonged the mean time-to-peak effect of 4α-PDD (314.3±63.5s) in comparison to non-BisX-treated cells (157.9±16.1s)^[3]. In human skin biopsies received transdermal injection of pemphigus vulgaris-IgG, treatment with BisX (1μM) one hour before the injection significantly reduced the number of desmosomes as compared to normal control samples (0.33 ± 0.05/μm vs. 0.69 ± 0.02/μm)^[4].

作用机制

Bisindolylmaleimide X HCl competes with ATP for binding to PKC^[5].

Bisindolylmaleimide X HCl 动物研究

Dose	Rat: 10 mg/kg - 50 mg/kg^[1] (p.o., BID); 10 mg/kg^[1] (i.v.)
Administration	p.o., i.v.

Bisindolylmaleimide X HCl 参考文献

[1]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt2)(Pt2):335-7.

[2]Brehmer D, Godl K, Zech B, Wissing J, Daub H. Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors. Mol Cell Proteomics. 2004 May;3(5):490-500.

[3]Xu F, Satoh E, Iijima T. Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4. Br J Pharmacol. 2003 Sep;140(2):413-21.

[4]Role of PKC and ERK Signaling in Epidermal Blistering and Desmosome Regulation in Pemphigus

[5]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt2)(Pt2):335-7.

Bisindolylmaleimide X HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.08mL

21.69mL

4.34mL

2.17mL

Bisindolylmaleimide X HCl 技术信息

CAS号	145317-11-9
分子式	C₂₆H₂₅ClN₄O₂
分子量	460.955

别名	BIM-X hydrochloride;Ro31-8425 hydrochloride;Ro 31-8425;BIM X;Bisindolylmaleimide X (hydrochloride);Bisindolylmaleimide X hydrochloride
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,2-8°C

溶解度

DMSO: 20 mg/mL(43.39 mM)，配合低频超声助溶，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

Bisindolylmaleimide X HCl {[allProObj[0].p_purity_real_show]}

Bisindolylmaleimide X HCl 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 X HCl 质控信息

Bisindolylmaleimide X HCl 生物活性

Bisindolylmaleimide X HCl 动物研究

Bisindolylmaleimide X HCl 参考文献

Bisindolylmaleimide X HCl 实验方案

Bisindolylmaleimide X HCl 技术信息

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Bisindolylmaleimide X HCl 实验方案

Bisindolylmaleimide X HCl 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 X HCl 纯度/质量文件产品仅供科研