Product overview

  • Name
    Cmpd101
  • Short description
    Novel, potent and selective GRK2/GRK3 inhibitor
  • Biological description

    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).

    Has no activity at GRK5 at concentrations up to 125 µM and shows little activity at a broad range of other kinases.

    Membrane permeable.

    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).

  • Alternative names
    Compound 101; Takeda compound 101
  • Biological action
    Inhibitor
  • 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

  • Our products in action

Images

Properties

  • 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]
  • 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

Storing and Using Your Product

  • Storage instructions
    -20°C
  • Solubility overview
    Soluble in DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for Cmpd101

  • Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.

    Thal et al (2011) Mol Pharmacol 80 : 294-303
    PubMedID: 21596927
  • 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
    PubMedID: 26013542
  • 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
    PubMedID: 26927499
  • Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.

    Urs et al (2016) Proc Natl Acad Sci U S A 113(50) : E8178-E8186
    PubMedID: 27911814
The following papers have cited the use of Cmpd101 (HB2840) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • 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
    PubMedID: 26927499
  • Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.

    Urs et al (2016) Proc Natl Acad Sci U S A 113(50) : E8178-E8186
    PubMedID: 27911814
  • G Protein-coupled Receptor Kinase 2 (GRK2) Promotes Breast Tumorigenesis Through a HDAC6-Pin1 Axis. [See Supplemental]

    Nogues et al(2016) EBioMedicine 132-145. : 13
    PubMedID: 27720394
  • Agonist-Dependent And -Independent Kappa Opioid Receptor Phosphorylation Showed Distinct Phosphorylation Patterns And Resulted In Different Cellular Outcomes

    Chiu et al(2017) bioRxiv https://doi.org/ : 10.1101/137570
  • Absence of dopamine D2-receptor modulation of NMDA responses in neonatal rat substantia nigra dopaminergic neurones

    Hosni et al(2016) J Physiol. Proc Physiol Soc 37 : PCA271
  • Muscarinic receptor regulates extracellular signal regulated kinase by two modes of arrestin binding.

    Jung et al(2017) Proc Natl Acad Sci U S A doi: 10.1073/pnas.1700331114 : pii: 201700331
    PubMedID: 28652372

Product FAQ's

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.

Reviews & Product Guides

Reviews

  • Verified customer, Pfizer

    Your Cmpd101 – worked great!
  • Verified customer, Monash University

    Your Cmpd101 behaved as expected