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Submit ReviewH-7 dihydrochloride
Description: Protein kinase inhibitor
Chemical Name: (±)-1-(5-Isoquinolinesulphonyl)-2-methylpiperazine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for H-7 dihydrochloride
H-7 dihydrochloride is a protein kinase inhibitor (IC50 values for inhibition of PKA, PKG, PKC and myosin light chain kinase are 3.0, 5.8, 6.0 and 97.0 μM, respectively. H-7 shows antiviral activity against influenza A (IC50 = 10 μM) in vitro. H-7 also inhibits interleukin-stimulated secretion of IgM and blocks PMA-stimulated interleukin 1β production.
Compound Libraries for H-7 dihydrochloride
H-7 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for H-7 dihydrochloride
| M. Wt | 364.29 |
| Formula | C14H17N3O2S.2HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 108930-17-2 |
| PubChem ID | 73332 |
| InChI Key | OARGPFMFRLLKPF-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CC1CNCCN1S(=O)(=O)C1=CC=CC2=CN=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for H-7 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 36.43 | 100 | |
| DMSO | 7.29 | 20 |
Preparing Stock Solutions for H-7 dihydrochloride
The following data is based on the product molecular weight 364.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.75 mL | 13.73 mL | 27.45 mL |
| 5 mM | 0.55 mL | 2.75 mL | 5.49 mL |
| 10 mM | 0.27 mL | 1.37 mL | 2.75 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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Product Datasheets for H-7 dihydrochloride
References for H-7 dihydrochloride
References are publications that support the biological activity of the product.
Hidaka et al (1984) Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 23 5036 PMID: 6238627
Quick et al (1992) The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source. Biochem.Biophys.Res.Commun. 187 657 PMID: 1530632
Ratz et al (1990) Effect of the kinase inhibitor, H-7, on stress, crossbridge phosphorylation, muscle shortening and inositol phosphate production in rabbit arteries. J.Pharmacol.Exp.Ther. 252 253 PMID: 2299593
Kurokawa et al (1990) Inhibitory effect of protein kinase C inhibitor on the replication of influenza type A virus. J.Gen.Virol. 71 2149 PMID: 1698925
Hurme et al (1990) Control of interleukin-1 beta expression by protein kinase C and cyclic adenosine monophosphate in myeloid leukemia cells Blood 76 2198 PMID: 2175219
If you know of a relevant reference for H-7 dihydrochloride, please let us know.
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Keywords: H-7 dihydrochloride, H-7 dihydrochloride supplier, Protein, kinase, Broad, Spectrum, inhibitors, inhibits, H7, dihydrochloride, Kinase, Inhibitors, Influenza, Viruses, 0542, Tocris Bioscience
4 Citations for H-7 dihydrochloride
Citations are publications that use Tocris products. Selected citations for H-7 dihydrochloride include:
Ludgate et al (2012) Cyclin-dependent kinase 2 phosphorylates s/t-p sites in the hepadnavirus core protein C-terminal domain and is incorporated into viral capsids. J Virol 86 12237 PMID: 22951823
Belmeguenai and Hansel (2005) A role for protein phosphatases 1, 2A, and 2B in cerebellar long-term potentiation. Mol Pharmacol 25 10768 PMID: 16291950
Zhao et al (2018) TRPV4 Blockade Preserves the Blood-Brain Barrier by Inhibiting Stress Fiber Formation in a Rat Model of Intracerebral Hemorrhage. Front Mol Neurosci 11 97 PMID: 29636662
Barcomb et al (2013) Enzymatic activity of CaMKII is not required for its interaction with the glutamate receptor subunit GluN2B. Front Mol Neurosci 84 834 PMID: 24056996
Do you know of a great paper that uses H-7 dihydrochloride from Tocris? Please let us know.
Reviews for H-7 dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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H7 was studied for its inhibitory role in cAMP dependent protein kinase.
By
Anonymous on 12/24/2019
Species: Human
H7 was studied for its inhibitory role in cAMP dependent protein kinase with ICso values of 18 and 16 gM respectively.
Cultures were incubated for 16 hours at 37 ~ in an atmosphere of 5% CO2 and 95% humidified air. 1~tCi of [3H]-thymidine was added to each well and cultures incubated for a further 5 hours. Cells were then harvested onto glass fibre filters, washed and incorporated radioactivity determined by liq- uid scintillation spectrometry.
