H-7 dihydrochloride

Name: H-7 dihydrochloride
Brand: Tocris Bioscience
SKU: 0542
Rating: 5 (1 reviews)

Catalog # 0542

Citations (4)

(1)

COA / SDS

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Key Product Details

Description:	Protein kinase inhibitor
Chemical Name:	(±)-1-(5-Isoquinolinesulphonyl)-2-methylpiperazine dihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	364.29

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Biological Activity

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

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

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	36.43	100
	DMSO	7.29	20

Preparing Stock Solutions

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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References

References are publications that support the biological activity of the product.

Quick The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source. Biochem.Biophys.Res.Commun. 1992 PMID: 1530632
Ratz Effect of the kinase inhibitor, H-7, on stress, crossbridge phosphorylation, muscle shortening and inositol phosphate production in rabbit arteries. J.Pharmacol.Exp.Ther. 1990 PMID: 2299593
Kurokawa Inhibitory effect of protein kinase C inhibitor on the replication of influenza type A virus. J.Gen.Virol. 1990 PMID: 1698925
Hurme Control of interleukin-1 beta expression by protein kinase C and cyclic adenosine monophosphate in myeloid leukemia cells Blood 1990 PMID: 2175219
Hidaka Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 1984 PMID: 6238627

Citations for H-7 dihydrochloride (4)

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Citations are publications that use Bio-Techne products. Selected citations for H-7 dihydrochloride include:

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
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

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H7 was studied for its inhibitory role in cAMP dependent protein kinase

Name: Anonymous

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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