Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 60.00 | |
5 mg | In stock | $ 128.00 | |
10 mg | In stock | $ 207.00 | |
25 mg | In stock | $ 418.00 | |
50 mg | In stock | $ 627.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 133.00 |
Description | CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. |
Targets&IC50 | PKCα:8.1 μM, ROCK2:1.4 μM, GRK2:18 nM, GRK3:5.4 nM |
In vitro | 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]. |
Molecular Weight | 466.46 |
Formula | C24H21F3N6O |
CAS No. | 865608-11-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (535.95 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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CMPD101 865608-11-3 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling GPCR/G Protein Stem Cells PKC GRK ROCK Rho-associated kinase Rho-kinase ROK desensitization Inhibitor inhibit CMPD-101 failure Neuron CMPD 101 Protein kinase C heart Rho-associated protein kinase inhibitor