1. Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
    Autophagy
  2. PKA
    Autophagy

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

Cat. No.: HY-15979A Purity: 98.94%
Data Sheet 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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 74 In-stock
10 mg USD 67 In-stock
50 mg USD 259 In-stock
100 mg USD 479 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of H-89 dihydrochloride:

    H-89 dihydrochloride purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.

    The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.

    H-89 dihydrochloride purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.

    The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.
    • 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 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
    Please refer to the solubility information to select the appropriate solvent.
    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.

    Purity: 98.94%

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

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