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  2. PKA Autophagy
  3. H-89

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

Size Price Stock Quantity
5 mg USD 43 In-stock
10 mg USD 67 In-stock
50 mg USD 259 In-stock
100 mg USD 440 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 99 publication(s) in Google Scholar

Other Forms of H-89:

Top Publications Citing Use of Products

94 Publications Citing Use of MCE H-89

WB
Proliferation Assay
RT-PCR

    H-89 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Jan 5.  [Abstract]

    H89 (5 μM; 6 h) reverses ISO (Isoprenaline hydrochloride)-triggered decreases in the mRNA levels of the IFNB1 gene, the expression of which has been induced by SeV infection, in THP1 cells.

    H-89 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2023 Apr 2,19.

    H-89 dihydrochloride (H-89; 10 μM; 2 h) blocks the epinephrine-induced phosphorylation of CREB1 in MC38 and HT-29 cells.

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

    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).

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

    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 MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.  [Abstract]

    The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

    MedChemExpress (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].

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

    Molecular Weight

    446.36

    Formula

    C20H20BrN3O2S

    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (224.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2403 mL 11.2017 mL 22.4034 mL
    5 mM 0.4481 mL 2.2403 mL 4.4807 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2403 mL 11.2017 mL 22.4034 mL 56.0086 mL
    5 mM 0.4481 mL 2.2403 mL 4.4807 mL 11.2017 mL
    10 mM 0.2240 mL 1.1202 mL 2.2403 mL 5.6009 mL
    15 mM 0.1494 mL 0.7468 mL 1.4936 mL 3.7339 mL
    20 mM 0.1120 mL 0.5601 mL 1.1202 mL 2.8004 mL
    25 mM 0.0896 mL 0.4481 mL 0.8961 mL 2.2403 mL
    30 mM 0.0747 mL 0.3734 mL 0.7468 mL 1.8670 mL
    40 mM 0.0560 mL 0.2800 mL 0.5601 mL 1.4002 mL
    50 mM 0.0448 mL 0.2240 mL 0.4481 mL 1.1202 mL
    60 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9335 mL
    80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.7001 mL
    100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5601 mL
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    H-89 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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