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H-89

Cat. No. M3559
H-89 Structure
Synonym:

Protein kinase inhibitor H-89

Size Price Availability Quantity
50mg USD 260  USD260 In stock
100mg USD 440  USD440 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
Source J Appl Oral Sci (2018). Figure 5. H-89
Method Western blotting
Cell Lines mDP cells
Concentrations 10 μM
Incubation Time 6 h
Results CaCl2-induced ERK1/2 phosphorylation was not inhibited in the presence H-89.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kaveh Tabrizian, et al. Tadalafil Reversed H-89 - and Scopolamine - Induced Spatial Learning Impairments in Male Rats

[2] Rojin Sharif, et al. Melatonin reverses H-89 induced spatial memory deficit: Involvement of oxidative stress and mitochondrial function

[3] Randi J Parks, et al. H-89 decreases the gain of excitation-contraction coupling and attenuates calcium sparks in the absence of beta-adrenergic stimulation

[4] Yoshiro Kato, et al. H-89 potentiates adipogenesis in 3T3-L1 cells by activating insulin signaling independently of protein kinase A

[5] Siyanda Makaula, et al. H-89, a non-specific inhibitor of protein kinase A, promotes post-ischemic cardiac contractile recovery and reduces infarct size

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Keywords: H-89, Protein kinase inhibitor H-89 supplier, PKA, inhibitors, activators

 
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