| Description | H-89 is a selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A; IC50: 48 nM). H-89 has weak inhibition on PKG, Casein Kinase, PKC, and other kinases. |
| In vitro | H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. 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.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. |
| In vivo | 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.H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. |
| Target activity | PKA:48 nM |
| Synonyms | Protein kinase inhibitor H-89 |
| molecular weight | 446.36 |
| Molecular formula | C20H20BrN3O2S |
| CAS | 127243-85-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Chijiwa T, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol Chem. 1990 Mar 25;265(9):5267-72. 2. Blazev R, et al. Effects of the PKA inhibitor H-89 on excitation-contraction coupling in skinned and intact skeletal muscle fibres. J Muscle Res Cell Motil. 2001;22(3):277-86. 3. Hosseini-Zare MS, et al. Effects of pentoxifylline and H-89 on epileptogenic activity of bucladesine in pentylenetetrazol-treated mice. Eur J Pharmacol. 2011 Nov 30;670(2-3):464-70. 4. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway[J]. International Journal of Molecular Medicine. 2021, 47(5): 1-11 |
| Citations | 1. Liu M, Yang Y, Tan B, et al. G αi and G βγ subunits have opposing effects on dexmedetomidine-induced sedation. European Journal of Pharmacology. 2018, 831: 28-37 2. Yu Z, Kong D, Liang Y, et al. Protective effects of VMY-2-95 on corticosterone-induced injuries in mice and cellular models. Acta Pharmaceutica Sinica B. 2021 3. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway. International Journal of Molecular Medicine. 2021 May;47(5):91. doi: 10.3892/ijmm.2021.4924. Epub 2021 Mar 31. |