CMPD101

生物活性靶点体外研究 CMPD101 试剂级价格

CMPD101

CAS号:865608-11-3
英文名:CMPD101
中文名:CMPD101
CBNumber:CB73345437
分子式:C24H21F3N6O
分子量:466.46
MOL File:865608-11-3.mol

CMPD101化学性质

熔点 :>80°C (dec.)
储存条件 :-20°C Freezer
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
颜色 :Off-White to Pale Yellow

CMPD101性质、用途与生产工艺

生物活性 CMPD101 是一种高效、高选择性、膜透性的 GRK2/3 小分子抑制剂，IC50 分别为 18 nM 和 5.4 nM。CMPD101 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。CMPD101 可用于心衰疾病的研究。

靶点

GRK2

18 nM (IC ₅₀ )

GRK3

5.4 nM (IC ₅₀ )

PKCα

8.1 μM (IC ₅₀ )

ROCK2

1.4 μM (IC ₅₀ )

体外研究

CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line. 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 Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues. CMPD101 (3-30 μM; pre-30 minutes) does not affect 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.

Western Blot Analysis

Cell Line:	HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration:	3 μM, 30 μM
Incubation Time:	Pre-30 minutes
Result:	Surpressed Ser375 expression completely at a high dose.

Western Blot Analysis

Cell Line:	HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration:	3 μM, 30 μM
Incubation Time:	Pre-30 minutes
Result:	Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression.