H7 dihydrochloride
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 540189

CAS#: 108930-17-2

Description: H7 is a specific protein kinase C inhibitor and protein kinase G inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.


Price and Availability

Size
Price

10mg
USD 190
Size
Price

25mg
USD 350
Size
Price

50mg
USD 650

H7 dihydrochloride, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 540189
Name: H7 dihydrochloride
CAS#: 108930-17-2
Chemical Formula: C31H42N6O5S
Exact Mass: 610.2937
Molecular Weight: 610.77
Elemental Analysis: C, 60.96; H, 6.93; N, 13.76; O, 13.10; S, 5.25


Synonym: H7 dihydrochloride; H7 HCl.

IUPAC/Chemical Name: 5-((2-methylpiperazin-1-yl)sulfonyl)isoquinoline dihydrochloride

InChi Key: OARGPFMFRLLKPF-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H17N3O2S.2ClH/c1-11-9-16-7-8-17(11)20(18,19)14-4-2-3-12-10-15-6-5-13(12)14;;/h2-6,10-11,16H,7-9H2,1H3;2*1H

SMILES Code: O=S(C1=CC=CC2=C1C=CN=C2)(N3C(C)CNCC3)=O.[H]Cl.[H]Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Quick J, Ware JA, Driedger PE. The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source. Biochem Biophys Res Commun. 1992 Sep 16;187(2):657-63. PubMed PMID: 1530623.

2: Zhang X, Simerly C, Hartnett C, Schatten G, Smithgall TE. Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells. Stem Cell Res. 2014 Nov;13(3 Pt A):379-89. doi: 10.1016/j.scr.2014.09.007. Epub 2014 Sep 30. PubMed PMID: 25305536; PubMed Central PMCID: PMC4252886.

3: Fallon RJ, Danaher M. The effect of staurosporine, a protein kinase inhibitor, on asialoglycoprotein receptor endocytosis. Exp Cell Res. 1992 Dec;203(2):420-6. PubMed PMID: 1459203.

4: Tsubaki M, Matsuoka H, Yamamoto C, Kato C, Ogaki M, Satou T, Itoh T, Kusunoki T, Tanimori Y, Nishida S. The protein kinase C inhibitor, H7, inhibits tumor cell invasion and metastasis in mouse melanoma via suppression of ERK1/2. Clin Exp Metastasis. 2007;24(6):431-8. Epub 2007 Jul 18. PubMed PMID: 17636410.

5: Kumahara E, Ebihara T, Saffen D. Protein kinase inhibitor H7 blocks the induction of immediate-early genes zif268 and c-fos by a mechanism unrelated to inhibition of protein kinase C but possibly related to inhibition of phosphorylation of RNA polymerase II. J Biol Chem. 1999 Apr 9;274(15):10430-8. PubMed PMID: 10187833.

6: Sluka KA, Willis WD. The effects of G-protein and protein kinase inhibitors on the behavioral responses of rats to intradermal injection of capsaicin. Pain. 1997 Jun;71(2):165-78. PubMed PMID: 9211478.

7: Hidaka H, Inagaki M, Kawamoto S, Sasaki Y. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41. PubMed PMID: 6238627.

8: Brodskiĭ VIa, Vasil'ev AV, Terskikh VV, Zvezdina ND, Fateeva VI, Mal'chenko LA, Kiseleva EV, Bueverova EI. [Mesenchymal stromal cells synchronize the rhythm of protein synthesis under the effect of an exogenous signal]. Ontogenez. 2012 May-Jun;43(3):229-32. Russian. PubMed PMID: 22834138.

9: Chen G, Steinmetz JE. Microinfusion of protein kinase inhibitor H7 into the cerebellum impairs the acquisition but not the retention of classical eyeblink conditioning in rabbits. Brain Res. 2000 Feb 21;856(1-2):193-201. PubMed PMID: 10677626.

10: Hirsh JK, Silinsky EM. Inhibition of spontaneous acetylcholine secretion by 2-chloroadenosine as revealed by a protein kinase inhibitor at the mouse neuromuscular junction. Br J Pharmacol. 2002 Apr;135(8):1897-902. PubMed PMID: 11959792; PubMed Central PMCID: PMC1573317.

11: Tokuyama S, Feng Y, Wakabayashi H, Ho IK. Possible involvement of protein kinases in physical dependence on opioids: studies using protein kinase inhibitors, H-7 and H-8. Eur J Pharmacol. 1995 Sep 15;284(1-2):101-7. PubMed PMID: 8549612.

12: Warrier A, Hjelmstad GO. Protein kinase inhibitors reduce GABA but not glutamate release in the nucleus accumbens. Neuropharmacology. 2007 Dec;53(8):925-9. Epub 2007 Sep 20. PubMed PMID: 17961609; PubMed Central PMCID: PMC2196408.

13: Robinson PJ, Cheng HC, Black CK, Schmidt CJ, Kariya T, Jones WD, Dage RC. MDL 27,032 [4-propyl-5-(4-pyridinyl)-2(3H)-oxazolone], an active site-directed inhibitor of protein kinase C and cyclic AMP-dependent protein kinase that relaxes vascular smooth muscle. J Pharmacol Exp Ther. 1990 Dec;255(3):1392-8. PubMed PMID: 2175806.

14: Klemm DJ, Kazim AL, Elias L. Phosphatidylglycerol-modulated protein kinase activity from human spleen. I. Enzyme purification and properties. Arch Biochem Biophys. 1988 Sep;265(2):496-505. PubMed PMID: 3421722.

15: Salathe M, Pratt MM, Wanner A. Protein kinase C-dependent phosphorylation of a ciliary membrane protein and inhibition of ciliary beating. J Cell Sci. 1993 Dec;106 ( Pt 4):1211-20. PubMed PMID: 7510301.

16: Li PM, Fukazawa H, Mizuno S, Uehara Y. Evaluation of protein kinase inhibitors in an assay system containing multiple protein kinase activities. Anticancer Res. 1993 Nov-Dec;13(6A):1957-64. PubMed PMID: 8297101.

17: Drews SJ, Hung F, Av-Gay Y. A protein kinase inhibitor as an antimycobacterial agent. FEMS Microbiol Lett. 2001 Dec 18;205(2):369-74. PubMed PMID: 11750829.

18: Ohtsuki M, Massagué J. Evidence for the involvement of protein kinase activity in transforming growth factor-beta signal transduction. Mol Cell Biol. 1992 Jan;12(1):261-5. PubMed PMID: 1729603; PubMed Central PMCID: PMC364090.

19: Fetscher C, Chen H, Schäfers RF, Wambach G, Heusch G, Michel MC. Modulation of noradrenaline-induced microvascular constriction by protein kinase inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2001 Jan;363(1):57-65. PubMed PMID: 11191837.

20: Mayes MA, Stogsdill PL, Prather RS. Parthenogenic activation of pig oocytes by protein kinase inhibition. Biol Reprod. 1995 Aug;53(2):270-5. PubMed PMID: 7492678.