A ROCK1 and GRK2 inhibitor
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GSK180736A

Item No. 26182

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide
CAS Number
817194-38-0
Molecular Formula
C19H16FN5O2
Formula Weight
365.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 70 mg/mLEthanol: 3 mg/mL
λmax
286 nm
SMILES
FC1=CC=C(C2NC(NC(C)=C2C(NC3=CC=C(NN=C4)C4=C3)=O)=O)C=C1
InChi Code
InChI=1S/C19H16FN5O2/c1-10-16(17(24-19(27)22-10)11-2-4-13(20)5-3-11)18(26)23-14-6-7-15-12(8-14)9-21-25-15/h2-9,17H,1H3,(H,21,25)(H,23,26)(H2,22,24,27)
InChi Key
HEAIGWIZTYAQTC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    GSK180736A is an inhibitor of Rho-associated kinase 1 (ROCK1; IC50 = 14 nM) and G protein-coupled receptor kinase 2 (GRK2; IC50 = 0.77 µM).1,2 It is selective for GRK2 over GRK1, GRK5, and PKA (IC50 = >100 µM for all) and selective for ROCK1 over RSK1 and p20S6K (IC50s = 3,100 and 2,850 nM, respectively).1,2 GSK180736A increases maximum contractility in isolated mouse cardiomyocytes when used at a concentration of 1 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Goodman, K.B., Cui, H., Dowdell, S.E., et al. Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J. Med. Chem. 50(1), 6-9 (2007).

    2. Waldschmidt, H.V., Homan, K.T., Cruz-Rodríguez, O., et al. Structure-based design, synthesis, and biological evaluation of highly selective and potent G protein-coupled receptor kinase 2 inhibitors. J. Med. Chem. 59(8), 3793-3807 (2016).