Product overview
| Name | Cmpd101 |
| Alternative names | Compound 101; Takeda compound 101 |
| Purity | >98% |
| Customer comments | We would recommend Cmpd 101 from Hello Bio – it performs exactly as expected in assays looking at MOPr desensitisation, phosphorylation and internalisation. Dr Chris Bailey, University of Bath, UK and author on Mol Pharmacol paper, PubMed ID 26013542 Your Cmpd101 – worked great! Dr Steven Gee, Pfizer Neuroscience, USA Your Cmpd101 behaved as expected. Verified customer, Monash University |
| Description | Novel, potent and selective GRK2/GRK3 inhibitor |
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Images
Inhibition of MOPr desensitization by Cmpd101
Figure A shows outward potassium currents recorded from rat LC neurons in response to a receptor saturating concentrations of, methionine enkephalin (Met Enk, 30 µM). Figure B shows currents induced by Met Enk in slices exposed to Cmpd101 (30 µM) for at least 15 min before and during the application of the opioid agonist.
Inhibition of DAMGO-induced MOPr phosphorylation by Cmpd101
Inhibition of DAMGO-induced MOPr phosphorylation by Cmpd101 HEK 293 cells stably expressing HA-tagged rat MOPr were pre-treated with Cmpd101 for 30 min prior to stimulation with DAMGO (10 µM for 5 min). Agonist-induced phosphorylation was assesed by Western Blot analysis using antibody targeting phospho-Ser375 (PS375). Anti-HA and anti-tubulin antibodies confirmed equal loading of the gels.
Inhibition of DAMGO-induced MOPr internalization by Cmpd101
Inhibition of DAMGO-induced MOPr internalisation by Cmpd101 Confocal images of HA-MOPrs following incubation with anti-HA antibody and fluorescein tagged secondary antibody (green), counterstained with Hoechst 33258 nucleic acid stain (blue) following incubation with DAMGO (10 µM) and/or Cmpd101 (30 µM). Images are from one experiment repeated 3 times. Scale bar= 10 µM
Cmpd101: Scientist Approved
Inhibition of MOPr desensitization by Cmpd101
Figure A shows outward potassium currents recorded from rat LC neurons in response to a receptor saturating concentrations of, methionine enkephalin (Met Enk, 30 µM). Figure B shows currents induced by Met Enk in slices exposed to Cmpd101 (30 µM) for at least 15 min before and during the application of the opioid agonist.
Inhibition of DAMGO-induced MOPr phosphorylation by Cmpd101
Inhibition of DAMGO-induced MOPr phosphorylation by Cmpd101 HEK 293 cells stably expressing HA-tagged rat MOPr were pre-treated with Cmpd101 for 30 min prior to stimulation with DAMGO (10 µM for 5 min). Agonist-induced phosphorylation was assesed by Western Blot analysis using antibody targeting phospho-Ser375 (PS375). Anti-HA and anti-tubulin antibodies confirmed equal loading of the gels.
Inhibition of DAMGO-induced MOPr internalization by Cmpd101
Inhibition of DAMGO-induced MOPr internalisation by Cmpd101 Confocal images of HA-MOPrs following incubation with anti-HA antibody and fluorescein tagged secondary antibody (green), counterstained with Hoechst 33258 nucleic acid stain (blue) following incubation with DAMGO (10 µM) and/or Cmpd101 (30 µM). Images are from one experiment repeated 3 times. Scale bar= 10 µM
Cmpd101: Scientist Approved
Biological Data
| Biological description | Cmpd101 (Compound 101) is a novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/GRK3) inhibitor (IC50 values are 35 and 32 nM at GRK2 and GRK3 respectively). Shows no activity at GRK5 at concentrations up to 125 µM and shows little activity at a broad range of other kinases. Membrane permeable. Cmpd101 can be used to study roles of GRK2/3 in GPCR desensitization and other functions. Shown to potentiate phosphatidylinositol 4,5-bisphosphate (PIP2) depletion and slow agonist-induced desensitization of protease-activated receptor 2 (PAR2). |
Solubility & Handling
| Storage instructions | -20°C |
| Solubility overview | Soluble in DMSO (100mM) |
| Handling | Hydroscopic solid, contact with air may cause material to become sticky. Product performance should not be affected but we recommend storing the material in a sealed jar. |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Purity | >98% |
| Chemical name | 3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride |
| Molecular Weight | 502.92 |
| Chemical structure | ![Cmpd101 [865608-11-3] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb2840.png "Cmpd101 [865608-11-3]") |
| Molecular Formula | C24H21N6OF3.HCl |
| CAS Number | 865608-11-3 |
| PubChem identifier | 11677079 |
| SMILES | CN1C(=NN=C1C2=CC=NC=C2)CNC3=CC=CC(=C3)C(=O)NCC4=CC=CC=C4C(F)(F)F |
| Source | Synthetic |
| InChi | InChI=1S/C24H21F3N6O/c1-33-21(31-32-22(33)16-9-11-28-12-10-16)15-29-19-7-4-6-17(13-19)23(34)30-14-18-5-2-3-8-20(18)24(25,26)27/h2-13,29H,14-15H2,1H3,(H,30,34) |
| InChiKey | WFOVEDJTASPCIR-UHFFFAOYSA-N |
| Appearance | Yellow solid |
Technical guides
Understanding purity and quality - a guide for life scientistsReferences for Cmpd101
References are publications that support the biological activity of the product
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Agonist-selective recruitment of engineered protein probes and of GRK2 by opioid receptors in living cells
Stoeber et al (2019) bioRxiv : https://doi.org/10.1101/866780 -
Contributions of protein kinases and β-arrestin to termination of protease-activated receptor 2 signaling.
Jung et al (2016) J Gen Physiol 147(3) : 255-71 -
Distinct cortical and striatal actions of a β-arrestin-biased D2 receptor ligand reveal unique antipsychotic-like properties.
Urs et al (2016) Proc Natl Acad Sci U S A 113(50) : E8178-E8186 -
Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization.
Lowe et al (2015) Mol Pharmacol 88(2) : 347-56 -
Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.
Thal et al (2011) Mol Pharmacol 80 : 294-303
Publications
These publications cite the use of Cmpd101 purchased from Hello Bio:
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The D2 receptor can directly recruit and activate GRK2 without G protein activation
Pack et al (2018) Journal of biological chemistry doi: 10.1074/ : jbc.RA117.001300 -
Regional Heterogeneity of D2-Receptor Signaling in the Dorsal Striatum and Nucleus Accumbens.
Marcott et al (2018) Neuron pii: S0896-6273(18)30244-7. : doi: 10.1016/j.neuron.2018.03.03PubMedID: 29656874 -
β-Arrestin Biased Signaling at the Dopamine D2 Receptor
Pack et al (2018) Dissertation : - -
Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid μ-opioid receptor desensitization.
Miess et al (2018) Sci Signal. 11(539) : pii: eaas9609PubMedID: 30018083 -
β-Arrestin Biased Signaling at the Dopamine D2 Receptor
Pack et al (2018) Duke University : Thesis
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