H-9 dihydrochloride

Names

[ Name ]:
H-9 dihydrochloride

[Synonym ]:
N-(2-Aminoethyl)-5-isoquinolinesulfonamide dihydrochloride
5-Isoquinolinesulfonamide, N-(2-aminoethyl)-, hydrochloride (1:2)
N-(2-Aminoethyl)isoquinoline-5-sulfonamide dihydrochloride
MFCD00069286

Biological Activity

[Description]:

H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines[1][2][3].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

Signaling Pathways >> Stem Cell/Wnt >> PKA

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

H-9 Dihydrochloride significantly inhibits A431 cells[1]. H-9 Dihydrochloride inhibits more effectively cyclic nucleotide-dependent protein kinases than other kinases[1].

[In Vivo]

H-9 Dihydrochloride microperfusion (100 μM) prevents picrotoxin seizures in 50% of the animals and significantly reduced the mean number of seizures and mean seizure duration[2].

[References]

[1]. Ito M, et al. A potent inhibitor of protein kinase C inhibits natural killer activity. Int J Immunopharmacol. 1988;10(3):211-6.

[2]. Vázquez-López A, et al. Role of cAMP-dependent protein kinase on acute picrotoxin-induced seizures. Neurochem Res. 2005 May;30(5):613-8.

[3]. Wollina U, et al. Inhibition of signal transduction in EGF-dependent epithelial cell lines. Int J Mol Med. 2003 Oct;12(4):673-7.

Chemical & Physical Properties

[ Melting Point ]:
250-255ºC dec.

[ Molecular Formula ]:
C₁₁H₁₅Cl₂N₃O₂S

[ Molecular Weight ]:
324.227

[ Exact Mass ]:
323.026215

[ PSA ]:
93.46000

[ LogP ]:
4.24780

[ Storage condition ]:
−20°C

Safety Information

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ WGK Germany ]:
3

[ HS Code ]:
2935009090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%