H 89 2HCl

Catalog No.S1582

H 89 2HCl Chemical Structure

Molecular Weight(MW): 519.28

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 310 In stock
USD 880 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

3 Customer Reviews

  • The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.

    J Cell Physiol, 2015, 230: 2233-2239. H 89 2HCl purchased from Selleck.

    (C): Representative photographs of western blot analysis of Bax and Bcl-2 levels. (D): Representative photographs of western blot of Caspase-3 levels.

    Eur J Pharm Sci, 2015, 70C: 82-91 . H 89 2HCl purchased from Selleck.

  • YAP localization was assessed by immunofluorescence assay after Forskolin or H 89 2HCl treatment. Scale bar: 50 μm.

    Sci Rep, 2016, 6:26835.. H 89 2HCl purchased from Selleck.

Purity & Quality Control

Choose Selective PKA Inhibitors

Biological Activity

Description H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.
Targets
PKA [1]
(Cell-free assay)
S6K1 [2]
(Cell-free assay)
48 nM(Ki) 80 nM
In vitro

H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with Ki of 48 nM, exhibits 10-fold selectivity over PKG, exhibits >500-fold selectivity over PKC, MLCK, calmodulin kinase II and casein kinase I/II. Pretreatment of the cells with H-89 (30 μM) 1 h before the addition of forskolin markedly inhibits the forskolin-induced protein phosphorylation in a dose-dependent manner. [1] H89 also 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. [2][3] H89 also has activity at some cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO  MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml6xNVAh|ryP M4fvcFEhcA>? MnfXbY5pcWKrdIOgOU1JXCCrbnT1Z4VlKGODTWCgdJJw\HWldHnvckBl\WO{ZXHz[S=> M{fZd|EzPTZ7ME[5
SK-N-MC NHHFT3JHfW6ldHnvckBCe3OjeR?= NVrrRWF2OzBizszN MlPZNlQhcA>? Mn\VSG1UVw>? NXq1bnFEemWmdXPld{B1cGViZH;3ck1z\We3bHH0bY9vKG:oIN8yNU1CWiCkeTDpd49xem:2ZYLlco9tKGK7IEWwKeKh M4XRelEyPzB3NEW0

... Click to View More Cell Line Experimental Data

In vivo H89 causes distinct modifications of protein phosphorylation, with the most robust changes in phosphorylation are fructose-1,6-biphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), NSFL1 cofactor p47, all which have potentially regulatory connections to cAMP/PKA. [5] H-89 (0.5, 1, 5 mg/kg) significantly attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice.[6]

Protocol

Kinase Assay:[1]
+ Expand

PKA enzyme activity:

cAMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HC1 (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cAMP or absence of cAMP, 3.3-20 μM [γ-32P]ATP (4 × 105 cpm), 0.5 μg of the enzyme, 100 μg of histone H2B, and each compound, as indicated.
Cell Research: [1]
+ Expand
  • Cell lines: PC12D
  • Concentrations: ~30 μM
  • Incubation Time: 1 h
  • Method: Levels of intracellular cAMP are determined. After 48 h in culture, PC12D 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.
    (Only for Reference)
Animal Research:[5] [6]
+ Expand
  • Animal Models: rat; mice
  • Formulation: Dissolved in 100% DMSO, diluted 1:20 in 0.9% sterile saline (Rat); 1% DMSO (Mice)
  • Dosages: 20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice)
  • Administration: s.c. (Rat); i.p. (Mice)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 104 mg/mL (200.27 mM)
Water 6 mg/mL (11.55 mM)
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 519.28
Formula

C20H20BrN3O2S.2HCl

CAS No. 130964-39-5
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Related PKA Products

Tags: buy H 89 2HCl | H 89 2HCl supplier | purchase H 89 2HCl | H 89 2HCl cost | H 89 2HCl manufacturer | order H 89 2HCl | H 89 2HCl distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID