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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.
| Molecular Weight | 446.36 |
| Formula | C20H20BrN3O2S |
| CAS Number | 127243-85-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PKA Products |
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| H-89 Dihydrochloride
H-89 dihydrochloride is a selective inhibitor of protein kinase A (PKA) with an IC50 value of 135 nM. |
| Bucladesine Sodium Salt
Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. |
| 8-Bromo-cAMP sodium salt
8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator. |
| 5-Iodotubercidin
5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. |
| HA-100
Ha-100 is a potent protein kinase inhibitor with IC50 values of 4 μM, 8 μM, 12 μM and 240 μM against PKG, PKA, PKC and MLC kinases, respectively. Ha-100 is also used as a ROCK inhibitor. |
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