化合物CMPD101 T14989

Product Introduction
Bioactivity


英文名: CMPD101

描述: CMPD101 是膜透性的 GRK2/3高选择性小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM，可研究心衰疾病。

体外活性: CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, significantly reduces the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line[1]. CMPD101 (3-30 μM; pre-30 minutes) does not influence the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30?μM. This compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375. Which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101and it also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 250 mg/mL (535.95 mM)


关键字: Rho-associated kinase | Rho-kinase | ROK | PKC | desensitization | Inhibitor | inhibit | CMPD-101 | failure | Neuron | CMPD 101 | ROCK | Protein kinase C | heart | Rho-associated protein kinase | CMPD101

相关产品: Narciclasine | Fasudil | GSK269962A | Merestinib dihydrochloride | ROCK-IN-7 | Rhodblock 6 | Ripasudil | AS 1892802 | Belumosudil | URMC-099

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neural Regeneration Compound Library | Inhibitor Library | Kinase Inhibitor Library | GPCR Compound Library | Epigenetics Compound Library | Highly Selective Inhibitor Library | TGF-beta/Smad Compound Library | Stem Cell Differentiation Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途