A PKA inhibitor
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H-89 (hydrochloride)

Item No. 10010556

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]5-isoquinolinesulfonamide, dihydrochloride
CAS Number
130964-39-5
Synonyms
  • 5-Isoquinolinesulfonamide
  • Protein Kinase Inhibitor H-89
Molecular Formula
C20H20BrN3O2S • 2HCl
Formula Weight
519.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 0.15 mg/ml
SMILES
O=S(C1=CC=CC2=CN=CC=C21)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl
InChi Code
InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;
InChi Key
GELOGQJVGPIKAM-WTVBWJGASA-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

    $238

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    50 mg

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    Product Description

    Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. H-89 is a potent, cell permeable inhibitor of PKA that demonstrates an IC50 value of 0.14 µM and a Ki value of 48 nM in standard kinase assays.1,2 While widely used to disrupt PKA signaling, the inhibitory activity of H-89 is non-selective. H-89 also inhibits S6K1, MSK1, ROCK2, PKBα, and MAPKAP-K1b with IC50 values of 0.08, 0.12, 0.27, 2.6, and 2.8 µM, respectively.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351(1), 95-105 (2000).

    2. Engh, R.A., Girod, A., Kinzel, V., et al. Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89 structural implications for selectivity. The Journal of Biological Chemisty 271(42), 26157-26164 (1996).

    Product Citations

    Sahoo, N., Gu, M., Zhang, X., et al. Gastric acid secretion from parietal cells is mediated by a Ca2+ efflux channel in the tubulovesicle. Dev. Cell 41(3), 262-273 (2017).