Ro 31-8220 mesylate | Ro 31-8220 methanesulfonate | PKC Inhibitor

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Ro 31-8220 甲磺酸盐 /Ro 31-8220 mesylate 99%+

货号：A350912 同义名： Ro 31-8220 methanesulfonate;Bisindolylmaleimide IX mesylate 产品仅供科研

Ro 31-8220 mesylate is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Ro 31-8220 mesylate 化学结构
CAS号：138489-18-6

Ro 31-8220 mesylate 3D分子结构
CAS号：138489-18-6

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Ro 31-8220 mesylate 纯度/质量文件

货号：A350912 标准纯度：99%+ 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: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 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								99%+
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		99%+
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									EGFR,PKA	95%
Dequalinium Chloride											99%+
Quercetin	✔									Src,Sirtuin	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。

Ro 31-8220 mesylate 生物活性

靶点	PKCε PKCε, IC50:24 nM PKCε PKCε, IC50:24 nM PKCε PKCε, IC50:24 nM PKCβ PKCβ2, IC50:14 nM PKCβ1, IC50:24 nM
描述	The protein kinase C (PKC) family consists of at least 12 serine-threonine kinases and can be classified into three major groups: classical, novel, and atypical. Under physiological conditions, activation PKC is a response to various growth factors^[3]. Ro 31-8220 Mesylate is a potent inhibitor with IC50 values of 5nM, 24nM, 14nM, 27nM and 24nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively^[4]. In vitro, treatment with 3 μM Ro 31-8220 Mesylate significantly increased Akt/PKB phosphorylation at Ser 473 within 60 mins in A549 cells^[5]. Ro 31-8220 Mesylate activated JNK1 with EC50 value of 2.3 nM. Ro 31-8220 Mesylate also inhibited growth factor-stimulated c-Fos expression and amplified c-Jun expression in Rat-1 fibroblasts^[6]. Ro 31-8220 Mesylate diminished the 17AAG-induced clearance ErbB2 from the cell surface at the concentration of 1 μM in SKBR-3 cells^[7]. Treatment of hippocampal slice prior to DHPG administration with Ro 31-8220 Mesylate at the concentration of 1 μM significantly reduced the baseline PPF ratio by approximately 7%, indicating that inhibiting basal PKC activity increased presynaptic release in WT mice^[8].
作用机制	Ro 31-8220 Mesylate carries a straight-chain alkyl side-chain bearing the cationic substituent which inhibits the PKC-α, PKC-β, PKC-γ and PKC-ε^[9].

Ro 31-8220 mesylate 参考文献

[1]Davies SP, Reddy H, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt1):95-105.

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

[3]Koivunen J, Aaltonen V, Peltonen J. Protein kinase C (PKC) family in cancer progression. Cancer Lett. 2006; 235(1): 1-10

[4]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993; 294:335-337

[5]Wen HC, Huang WC, Ali A, Woodgett JR, Lin WW. Negative regulation of phosphatidylinositol 3-kinase and Akt signaling pathway by PKC. Cell Signal. 2003; 15(1): 37-45

[6]Beltman J, McCormick F, Cook SJ. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996;271(43):27018-27024

[7]Bailey TA, Luan H, Tom E, et al. A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells. J Biol Chem. 2014;289(44):30443-30458

[8]Choi B, Lee HW, Mo S, et al. Inositol 1,4,5-trisphosphate 3-kinase A overexpressed in mouse forebrain modulates synaptic transmission and mGluR-LTD of CA1 pyramidal neurons. PLoS One. 2018;13(4):e0193859

[9]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993; 294:335-337

Ro 31-8220 mesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.03mL

1.81mL

0.90mL

18.06mL

3.61mL

1.81mL

Ro 31-8220 mesylate 技术信息

CAS号	138489-18-6
分子式	C₂₆H₂₇N₅O₅S₂
分子量	553.653

别名	Ro 31-8220 methanesulfonate;Bisindolylmaleimide IX mesylate;Ro 31-8220;BIM IX;Bisindolylmaleimide IX (mesylate);Bisindolylmaleimide IX
运输	蓝冰

存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(63.22 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

Ro 31-8220 甲磺酸盐 /Ro 31-8220 mesylate 99%+

Ro 31-8220 mesylate 纯度/质量文件

全球学术期刊中引用的产品

Ro 31-8220 mesylate 生物活性

Ro 31-8220 mesylate 参考文献

Ro 31-8220 mesylate 实验方案

Ro 31-8220 mesylate 技术信息

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PKCε	PKCε, IC50:24 nM
PKCε	PKCε, IC50:24 nM
PKCε	PKCε, IC50:24 nM
PKCβ	PKCβ2, IC50:14 nM PKCβ1, IC50:24 nM
PKCβ	PKCβ2, IC50:14 nM PKCβ1, IC50:24 nM
PKCβ	PKCβ2, IC50:14 nM PKCβ1, IC50:24 nM
PKCα	PKCα, IC50:5 nM
PKCα	PKCα, IC50:5 nM
PKCα	PKCα, IC50:5 nM
PKCγ	PKCγ, IC50:27 nM
PKCγ	PKCγ, IC50:27 nM
PKCγ	PKCγ, IC50:27 nM

Ro 31-8220 甲磺酸盐 /Ro 31-8220 mesylate 99%+

Ro 31-8220 mesylate 纯度/质量文件

全球学术期刊中引用的产品

Ro 31-8220 mesylate 生物活性

Ro 31-8220 mesylate 参考文献

Ro 31-8220 mesylate 实验方案

Ro 31-8220 mesylate 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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