Cat. No. 5642
Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,
Biological ActivityPotent and selective GRK2/3 inhibitor (IC50 values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Lowe et al (2015) Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 88 347. PMID: 26013542.
Thal et al (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 80 294. PMID: 21596927.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses CMPD101 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: CMPD101, supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Tocris Bioscience, G Protein (Heterotrimeric) Inhibitor products
Find multiple products by catalog number
New Products in this Area
High affinity caveolin-1 ligandSAG 21k
Hedgehog signaling activator; brain penetrant and orally bioavailable
April 10 - 13, 2017