A GRK6 inhibitor
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GRK6-IN-1

Item No. 46246

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-[(4-chloro-2-methoxyphenyl)methyl]-N4-(5-ethyl-1H-pyrazol-3-yl)-5-methoxy-2,4-quinazolinediamine
CAS Number
2677786-61-5
Synonyms
  • G Protein-coupled Receptor Kinase 6-IN-1
  • G Protein-coupled Receptor Kinase 6 Inhibitor 1
  • GRK6 Inhibitor 1
Molecular Formula
C22H23ClN6O2
Formula Weight
438.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CCC1=CC(NC2=NC(NCC3=CC=C(Cl)C=C3OC)=NC4=C2C(OC)=CC=C4)=NN1
InChi Code
InChI=1S/C22H23ClN6O2/c1-4-15-11-19(29-28-15)26-21-20-16(6-5-7-17(20)30-2)25-22(27-21)24-12-13-8-9-14(23)10-18(13)31-3/h5-11H,4,12H2,1-3H3,(H3,24,25,26,27,28,29)
InChi Key
ACLLLJSNOCYQOJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    GRK6-IN-1 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6).1,2 It reduces the proliferation of Hep3B and HCCLM3 hepatocellular carcinoma cells (IC50s = 3.25 and 2.87 µM, respectively).2 GRK6-IN-1 induces cell cycle arrest at the G1 phase in Hep3B and HCCLM3 cells and inhibits the migration and invasion of the same cells. It reduces tumor weight in Hep3B and HCCLM3 mouse xenograft models at 25 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Uehling, D.E., Joseph, B., Chung, K.C., et al. Correction to "Design, synthesis, and characterization of 4-aminoquinazolines as potent Inhibitors of the G protein-coupled receptor kinase 6 (GRK6) for the treatment of multiple myeloma". J. Med. Chem. 65(1), 886-887 (2021).

    2. Lin, J., Lin, J., Wang, X., et al. Suppression of GRK6 inhibits hepatocellular carcinoma progression by arresting the cell cycle. Tissue Cell 103, 103669 (2026).