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H-89 dihydrochloride (Synonyms: Protein kinase inhibitor H-89 dihydrochloride)

Cat. No.: HY-15979A Purity: 98.71%
SDS Handling Instructions

H-89 (dihydrochloride) is a potent inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.

For research use only. We do not sell to patients.
H-89 dihydrochloride Chemical Structure

H-89 dihydrochloride Chemical Structure

CAS No. : 130964-39-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $62 In-stock
10 mg $56 In-stock
50 mg $216 In-stock
100 mg $399 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of H-89 dihydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

H-89 (dihydrochloride) is a potent inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.

IC50 & Target

IC50: 48 nM (protein kinase A)

In Vitro

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. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates[1]. 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 Ca2+-sensitivity of the contractile apparatus in rat skinned fibres[2].

In Vivo

H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. 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[3].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9257 mL 9.6287 mL 19.2574 mL
5 mM 0.3851 mL 1.9257 mL 3.8515 mL
10 mM 0.1926 mL 0.9629 mL 1.9257 mL
Kinase Assay
[1]

Kinase activities are assayed at 30°C for 2-5 min by measuring the transfer of 32P from [γ-32P]ATP to substrates. The reaction is terminated by adding 1 mL of 20% trichloroacetic acid, following the addition of 100 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 rpm for 10 min, the pellet is resuspended in 5% trichloroacetic acid solution, the final pellet is dissolved in 1 mL of 1 N NaOH and the radioactivity is measured in a liquid scintillation counter. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

After 48 h in culture, PCl2D cells are cultured in test medium containing 30 μM H-89 for 1 h and then exposed to fresh medium that contained both 10 μM forskolin and 30 μM H-89. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5 mL of 6% trichloroacetic acid. To extract trichloroacetic acid, 2 mL of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

H-89 is dissolved in DMSO and distilled water (10%).

Male albino mice weighing 20-25 g are obtained. Pentoxifylline (25, 50, 100 mg/kg), bucladesine (50, 100, 300 nM/mouse) and H-89 (0.05, 0.1, 0.2 mg/100 g) are administered intraperitoneally (i.p.) 30 min before intravenous (i.v.) infusion of PTZ. In combination groups, the first and second components are injected 45 and 30 min before PTZ infusion. In all groups, the respective control animalsreceive an appropriate volume of vehicle. For the i.v. infusion, the needle is inserted into the lateral tail vein, fixed to the tail vein by a narrow piece of adhesive tape, and the animal is allowed to move freely. PTZ solution is infused at a concentration rate of 1 mL/min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

519.28

Formula

C₂₀H₂₂BrCl₂N₃O₂S

CAS No.

130964-39-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 50 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
H-89 dihydrochloride
Cat. No.:
HY-15979A
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