H-7 dihydrochloride

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Description: Protein kinase inhibitor
Chemical Name: (±)-1-(5-Isoquinolinesulphonyl)-2-methylpiperazine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

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

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


Do you know of a great paper that uses H-7 dihydrochloride from Tocris? Please let us know.

Reviews for H-7 dihydrochloride

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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.

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