SKU : MC515843
CAS Number : 127243-85-0
Molecular Formula : C20H20BrN3O2S | Molecular Weight : 446.36
Synonyms : Protein kinase inhibitor H-89
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | H-89 |
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CAS Number | 127243-85-0 |
MDL Number | MFCD00214119 |
Molecular Formula | C20H20BrN3O2S |
Molecular Weight | 446.36 |
Synonyms | Protein kinase inhibitor H-89 |
H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases. IC50 & Target: IC50: 48 nM (protein kinase A) 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 Ca32-sensitivity of the contractile apparatus in rat skinned fibres[2]. 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].
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