1. Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
    Autophagy
  2. PKA
    Autophagy
  3. H-89

H-89 

Cat. No.: HY-15979
Handling Instructions

H-89 is a potent and selective 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 Chemical Structure

H-89 Chemical Structure

CAS No. : 127243-85-0

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Top Publications Citing Use of Products

    H-89 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.

    H-89 purchased from MCE. Usage Cited in: Infect Immun. 2018 Dec 19;87(1). pii: e00508-1

    J774A.1 cells are pre-treated with 473 U0126 (10 μM), SB208530 (10 μM), SP600125 (10 μM), or H89 (50 μM), then infected with ΔeseH E. piscicida at the MOI of 10 for 3.5 h. Cell lysates were probed with anti-phospho-p65 (Ser276), anti-p65, and anti-β-actin antibodies.

    H-89 purchased from MCE. Usage Cited in: Aging (Albany NY). 2018 Jul 24;10(7):1722-1744.

    Expressions of p-eNOS (Ser1177) and total eNOS are measured in HUVECs treated with or without H2O2 and Hemin in the presence or absence of Akt inhibitor MK-2206, PKA inhibitor H-89 or AMPK inhibitor Compound C (CP-C).
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    Description

    H-89 is a potent and selective 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 Ca32-sensitivity of the contractile apparatus in rat skinned fibres[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    446.36

    Formula

    C₂₀H₂₀BrN₃O₂S

    CAS No.

    127243-85-0

    SMILES

    O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    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]

    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
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    Keywords:

    H-89H89H 89PKAAutophagyProtein kinase AInhibitorinhibitorinhibit

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