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H-89

Catalog No. T11524 CAS 127243-85-0

Synonyms: Protein kinase inhibitor H-89

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.

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H-89, CAS 127243-85-0

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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.
Targets&IC50	PKA:48 nM
In vitro	H-89, at varying concentrations, impacts cellular processes through distinct mechanisms. At 30 μM, it significantly suppresses cAMP-dependent histone IIb phosphorylation in PC12D cell lysates. At lower doses (1-2 μM), it notably decelerates the repriming rate in rat skinned fibers, likely by negatively affecting the T-system potential. Higher concentrations (10-100 μM) restrict net Ca2+ uptake by the sarcoplasmic reticulum (SR) and alter the Ca^32+-sensitivity of the contractile apparatus in these fibers. H-89 also acts as a competitive inhibitor of protein kinase A against ATP, leading to a dose-dependent blockade of forskolin-induced protein phosphorylation without reducing intracellular cyclic AMP levels in PC12D cells. Moreover, it significantly hampers forskolin-induced neurite outgrowth from PC12D cells, showcasing its broad inhibitory effects on cellular signaling and function.
In vivo	H-89 administered intraperitoneally at doses of 0.05 and 0.2 mg/100g inhibits the epileptogenic effects induced by bucladesine (300 nM), significantly elevating both seizure latency and seizure threshold. Additionally, a dose of 0.2 mg/100g of H-89 significantly enhances seizure latency and threshold in animals treated with PTZ.

Synonyms	Protein kinase inhibitor H-89
Molecular Weight	446.36
Formula	C20H20BrN3O2S
CAS No.	127243-85-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

H-89 127243-85-0 Others Protein kinase inhibitor H-89 H89 H 89 inhibitor inhibit

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