CMPD101
CMPD101 用途与合成方法
|
GRK2 18 nM (IC 50 ) |
GRK3 5.4 nM (IC 50 ) |
PKCα 8.1 μM (IC 50 ) |
ROCK2 1.4 μM (IC 50 ) |
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. |
CMPD101 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-04-30 | HY-103045 | 5 mg | 1600 | ||
| 2024-04-30 | HY-103045 | CMPD101 | 865608-11-3 | 10mM * 1mLin DMSO | 1642 |
