CMPD101
Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
Purity: ≥98%
Biological Activity
CMPD101 is a potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.
Thal et al.
Mol.Pharmacol., 2011;80:294 -
Design, synthesis, and evaluation of the highly selective and potent G-protein-coupled receptor kinase 2 (GRK2) inhibitor for the potential treatment of heart failure.
Okawa et al.
J.Med.Chem., 2017;60:6942 -
Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization.
Lowe et al.
Mol.Pharmacol., 2015;88:347
Product Datasheets
Citations for CMPD101
The citations listed below are publications that use Tocris products. Selected citations for CMPD101 include:
7 Citations: Showing 1 - 7
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Subcellular location defines GPCR signal transduction.
Authors: Francesco Luigi Et al.
Sci Adv 2023;9:eadf6059
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Mechanisms of differential desensitization of metabotropic glutamate receptors.
Authors: Joshua Et al.
Cell Rep 2021;35:109050
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Biological characterization of ligands targeting the human CC chemokine receptor 8 (CCR8) reveals the biased signaling properties of small molecule agonists.
Authors: Dominique Et al.
Biochem Pharmacol 2021;188:114565
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Mechanical and chemical activation of GPR68 probed with a genetically encoded fluorescent reporter.
Authors: Miou Et al.
J Cell Sci 2021;134
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Mutations in GRK2 cause Jeune syndrome by impairing Hedgehog and canonical Wnt signaling.
Authors: Jiri Et al.
EMBO Mol Med 2020;12:e11739
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A Discrete Presynaptic Vesicle Cycle for Neuromodulator Receptors.
Authors: Mark Et al.
Neuron 2020;105:663-677.e8
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Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor.
Authors: Reyes-Alcaraz Et al.
Commun Biol 2018;1:128
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