A ROCK inhibitor
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GSK429286A

Item No. 15262

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(6-fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
CAS Number
864082-47-3
Molecular Formula
C21H16F4N4O2
Formula Weight
432.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
282, 362 nm
SMILES
O=C1NC(C)=C(C(NC2=C(F)C=C(NN=C3)C3=C2)=O)C(C4=CC=C(C(F)(F)F)C=C4)C1
InChi Code
InChI=1S/C21H16F4N4O2/c1-10-19(20(31)28-17-6-12-9-26-29-16(12)8-15(17)22)14(7-18(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-6,8-9,14H,7H2,1H3,(H,26,29)(H,27,30)(H,28,31)
InChi Key
OLIIUAHHAZEXEX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $38

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    Product Description

    GSK429286A is a cell-permeable inhibitor of Rho-associated kinase (IC50 = 14 nM).1 It less potently inhibits p90 and p70 ribosomal S6 kinases (IC50s = 780 and 1,940 nM, respectively) and is ineffective against leucine-rich repeat protein kinase-2.1,2 GSK429286A reverses adrenalin-induced contraction of rat aortic rings (IC50 = 190 nM) and produces a dose-dependent decrease in mean arterial pressure in spontaneously-hypertensive rats.1

    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. Nichols, R.J., Dzamko, N., Hutti, J.E., et al. Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson’s disease. Biochem. J. 424(1), 47-60 (2009).