H-89

Brand

No Brand

Description

H-89 is a potent and selective inhibitor of PKA, with an IC50 of about 50 nM. H-89 inhibits several other kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, respectively. H-89 also inhibits PKG and the µ isotype of PKC (at about 500 nM). In contrast, most other PKC isotypes are much more weakly inhibited, with IC50’s in the 32 µM range. Intraperitoneal administration of H-89 (0.2 mg/100g) significantly increased seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100g) prevented the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.

Application

Reactivity

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