Technical documents: SDS CoA Datasheet

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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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.



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More Info

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
Molecular Formula C24H21N6OF3.HCl
CAS Number 865608-11-3
PubChem identifier 11677079
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)
Appearance Yellow solid


How do I make a 30 uM concentration of Cmpd101 in aCSF, from an initial stock made in 100% DMSO?

If you prepare a stock solution of Cmpd101 dissolved in 100% DMSO to a concentration of 10-30 mM, you should then be able to take the final concentration down to 30 uM in ACSF (final DMSO 0.1%).

How do I solubilise (dissolve) Cmpd101?

You can solubilise Cmpd101 in DMSO, up to a concentration of 100 mM.
Once Cmpd101 is in suspension, if you have problems solubilising it, you can try:

  • Stirring – try rapidly stirring or vortexing in a whirlimixer
  • Heating – try warming it gently in a water bath
  • Sonicating – sonication may also be worth a try   

Temperature is very important when solubilising biochemicals. For example if you’ve cooled or frozen your Cmpd101 solution, it may have precipitated out of solution. So here’s an important rule – make sure you check that Cmpd101 is fully re-dissolved before use.

Do I need to re-weigh the Cmpd101 in my vial?

Yes - you should weigh out the quantity of Cmpd101 that you require for your experiment as the amount of product in our vials isn’t weighed out accurately enough for direct addition of solution. There are some exceptions to this but if this is the case, it will be stated clearly on the datasheet.

How do I store Cmpd101?

Storing Cmpd101 as a solid: If you keep the vial kept tightly sealed at room temperature, you can store Cmpd101 for up to 6months.

Storing and working with solutions of Cmpd101:
If you are planning on storing and working with solutions of Cmpd101, we recommend preparing and using your solutions on the same day. However, if this isn’t possible and you need to prepare stock solutions of Cmpd101  beforehand, you should aliquot out the solution into tightly sealed vials at store at -20°C. We generally recommend that these will be useable for up to one month. You should also allow Cmpd101 to equilibrate to RT for at least one hour before opening and using.

References for Cmpd101

References are publications that support the biological activity of the product
  • Agonist-selective recruitment of engineered protein probes and of GRK2 by opioid receptors in living cells

    Stoeber et al (2019) bioRxiv :
  • 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

5 Item(s)

These publications cite the use of Cmpd101 purchased from Hello Bio:
  • Endocytic trafficking determines cellular tolerance of presynaptic opioid signaling

    von Zastrow et al (2022) Biorxiv :
  • SGIP1 modulates kinetics and interactions of the cannabinoid receptor 1 and G protein-coupled receptor kinase 3 signalosome

    Gazdarica M et al (2022) J Neurochem 160(6) : 625-642
    PubMedID: 34970999
  • GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation.

    Todd NK et al (2022) Cell reports 40 : 111110
    PubMedID: 35858570
  • Persistent inflammation promotes endocannabinoid release and presynaptic cannabinoid 1 receptor desensitization

    Ingram et al (2022) Biorxiv :
  • A PKA Inhibitor Motif within Smoothened Controls Hedgehog Signal Transduction

    Myers et al (2021) bioRxiv : doi

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