A potent, nonspecific kinase inhibitor
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H-8 (hydrochloride)

Item No. 10010249

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide, dihydrochloride
CAS Number
113276-94-1
Synonyms
  • Protein Kinase Inhibitor H-8
Molecular Formula
C12H15N3O2S • 2HCl
Formula Weight
338.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
217, 276, 324 nm
SMILES
CNCCNS(C1=CC=CC2=CN=CC=C21)(=O)=O.Cl.Cl
InChi Code
InChI=1S/C12H15N3O2S.2ClH/c1-13-7-8-15-18(16,17)12-4-2-3-10-9-14-6-5-11(10)12;;/h2-6,9,13,15H,7-8H2,1H3;2*1H
InChi Key
RJJLZYZEVNCZIW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $41

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    10 mg

    $65

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    25 mg

    $128

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    50 mg

    $215

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    Product Description

    H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.1,2,3 H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).

    2. Hidaka, H., Inagaki, M., Kawamoto, S., et al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 23(21), 5036-5041 (1984).

    3. Hagiwara, M., Inagaki, M., and Hidaka, H. Specific binding of a novel compound, N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide (H-8) to the active site of cAMP-dependent protein kinase. Mol. Pharmacol. 31, 523-528 (1987).

    4. Rickert, P., Corden, J.L., and Lees, E. Cyclin C/CDK8 and cyclin H/CDK7/p36 are biochemically distinct CTD kinases. Oncogene 18(4), 1093-1102 (1999).