CMPD101 | GRK2/3 Inhibitor | AmBeed-信号通路专用抑制剂

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CMPD101 {[allProObj[0].p_purity_real_show]}

货号：A1165861

CMPD101是一种选择性 GRK2/3 抑制剂，对 GRK2 和 GRK3 的 IC50 分别为 32 nM 和 54 nM，用于心力衰竭等疾病的研究。

CMPD101 化学结构
CAS号：865608-11-3

CMPD101 3D分子结构
CAS号：865608-11-3

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CMPD101 纯度/质量文件产品仅供科研

货号：A1165861 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: • Nature, 2025. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Nat. Mater., 2025, 24, 1116-1125. Ambeed. [ A141030 , A131652 ]; • Nat. Electron., 2025, 8, 66-74. Ambeed. [ A100095 ]; • Nano-Micro Lett., 2025, 17, 311. Ambeed. [ A971305 ]; 更多 >

ROCK 亚型比较
转化生长因子-β 亚型比较
PKC 亚型比较

产品名称	ROCK ↓ ↑	ROCK1 ↓ ↑	ROCK2 ↓ ↑	其他靶点	纯度
Thiazovivin	+ ROCK, IC50: ~0.5 μM				98%
Netarsudil HCl	++++ ROCK, Ki: 2 nM				99%+
Y-33075 2HCl	++++ ROCK, IC50: 3.6 nM				99%+
ROCK1-IN-1	++ ROCK, Ki: 17nM				95%
GSK429286A		+++ ROCK1, IC50: 14 nM	++ ROCK2, IC50: 63 nM		99%+
Ripasudil		++ ROCK1, IC50: 51 nM	++ ROCK2, IC50: 19 nM		99%+
Belumosudil			++ ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM		99%+
Y-27632 2HCl		++ ROCK1, Ki: 140 nM	+ ROCK2, Ki: 300 nM		99%+
Fasudil HCl			+ ROCK2, Ki: 330 nM	PKG,Rho	98%
Chroman 1		++++ ROCK1, IC50: 52 pM	++++ ROCK2, IC50: 1 pM		99%
BAY-549		++++ ROCK1, IC50: 0.6 nM	++++ ROCK2, IC50: 1.1 nM		99%+
AT13148		+++ ROCK1, IC50: 6 nM	+++ ROCK2, IC50: 4 nM	PKA	95%
RKI-1447		+++ ROCK1, IC50: 14.5 nM	+++ ROCK2, IC50: 6.2 nM		99%+
Hydroxyfasudil HCl		+ ROCK1, IC50: 0.73 μM	+ ROCK2, IC50: 0.72 μM	PKA	98%
H-1152 2HCl			+++ ROCK2, IC50: 0.0120 μM	PKG	99%
GSK269962A HCl		++++ ROCK1, IC50: 1.6 nM	+++ ROCK2, IC50: 4 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	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%
(E/Z)-SIS3 free base						✔				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	✔									Src,Sirtuin	95%
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。

CMPD101 生物活性

描述

CMPD101 is a potent, highly selective, membrane-permeable small molecule inhibitor of GRK2/3, with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 is less selective for GRK1, GRK5, ROCK-2 and PKCα, with IC50s of 3.1 μM, 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used in heart failure studies ^[1].Pre-treatment of CMPD101 at a concentration of 100 μM for 20 minutes inhibits β2AR internalisation, significantly reduces isoproterenol-induced formation of lattice protein-encapsulated vesicles and β2AR-GFP fusion proteins are retained at the plasma membrane of the HEK-B2 cell line ^[1].Pre-treatment with CMPD101 in the concentration range of 3-30 μM for 30 min partially inhibited Ser375 phosphorylation, and pre-treatment with 30 μM CMPD101 completely blocked Ser375 phosphorylation. It also inhibited the phosphorylation of MOPr Thr370, Thr376 and Thr379 residues. Meanwhile, pre-treatment with CMPD101 in the concentration range of 3-30 μM for 30 min did not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, whereas at 30 μM, CMPD101 resulted in a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPs^[2].

CMPD101 参考文献

[1]Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.

[2]Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19.

CMPD101 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.44mL

4.29mL

2.14mL

CMPD101 技术信息

CAS号	865608-11-3
分子式	C₂₄H₂₁F₃N₆O
分子量	466.46
SMILES Code	CN1C(CNC2=CC(C(NCC3=C(C(F)(F)F)C=CC=C3)=O)=CC=C2)=NN=C1C4=CC=NC=C4
MDL No.	MFCD30182336

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 250 mg/mL(535.95 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：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

方案三

CMPD101 {[allProObj[0].p_purity_real_show]}

CMPD101 纯度/质量文件产品仅供科研

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CMPD101 {[allProObj[0].p_purity_real_show]}

CMPD101 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

CMPD101 质控信息

CMPD101 生物活性

CMPD101 参考文献

CMPD101 实验方案

CMPD101 技术信息

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大规格询价

摩尔计算器

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总药量计算器

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临床研究

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