H-89 2HCl

  Cat. No.:  DC7835   Featured
Chemical Structure
130964-39-5
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More than 5000 active chemicals with high quality for research!
Field of application
H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.
Cas No.: 130964-39-5
Chemical Name: 5-Isoquinolinesulfonamide,N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]-, hydrochloride (1:2)
Synonyms: 5-Isoquinolinesulfonamide,N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]-, hydrochloride (1:2);N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinoline Sulfonamide Dihydrochloride;H-89 dihydrochloride hydrate;H 89 2HCl;5-Isoquinolinesulfonamide,N-[2-[[3-(4-bromophenyl)-2-propen-1-yl]amino]ethyl]-, hydrochloride ...;H 89 dihydrochloride;H-89, Dihydrochloride;Protein kinase inhibitor H-89 dihydrochloride;H-89 hydrate dihydrochloride;(E)-N-(2-(4-bromocinnamylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride;(E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride;N-[2-[[3-(4-BroMophenyl)-2-propen-1-yl]aMino]ethyl]-5-isoquinolinesulfonaMide Hydrochloride;5-IsoquinolinesulfonaMide, N-[2-[[3-(4-broMophenyl)-2-propenyl]aMino]ethyl]-, dihydrochloride;N-[2-[[3-(4-Bromophenyl)-2-Propen-1-Yl]Amino]Ethyl]-5-Isoquinolinesulfonamide Hydrochloride (1:2);H-89 Dihydrochloride Hydrate,N-[2-(P-Bromocinnamylamino)Et;H-89 dihydrochloride
SMILES: O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl
Formula: C20H24BrCl2N3O3S
M.Wt: 537.297861099243
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: H-89 dihydrochloride is a potent inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
In Vivo: H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold[3].
In Vitro: H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates[1]. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca2+ uptake by the SR and affectes the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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