Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Targets |
PKA (Ki = 48 nM); S6K1 (IC50 = 80 nM); PKG (Ki = 0.48 μM)
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ln Vitro |
orskolin-induced protein phosphorylation is markedly and dose-dependently inhibited by pretreating the cells with H-89 (30 M) 1 hour before the addition of forskolin. [1] Other kinases that are inhibited by H89 include S6K1, MSK1, PKA, ROCKII, PKB, and MAPKAP-K1b, with IC50 values of 80, 120, 135, 270, 2600, and 2800 nM, respectively. [2] [3] Several cellular receptors and ion channels, including Kv1.3 K+ channels, 1AR, and 2AR, are also active in response to H89.[4] Forskolin-induced protein phosphorylation is markedly and dose-dependently inhibited by pretreating the cells with H-89 (30 M) 1 hour before the addition of forskolin. [1] Other kinases that are inhibited by H89 include S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, with IC50 values of 80, 120, 135, 270, 2600, and 2800 nM, respectively. [2] [3] Several cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR., are also active in response to H89. [4]
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ln Vivo |
The protein phosphorylation of H89 is altered in a variety of ways, but fructose-1,6-bisphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), and NSFL1 cofactor p47 exhibit the strongest phosphorylation changes. These proteins may all have regulatory relationships with cAMP/PKA. [5]
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Enzyme Assay |
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.
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Cell Assay |
Levels of intracellular cAMP are determined. After 48 hours of culture, PC12D cells are grown for 1 hour in test medium containing 30 μM H-89 before being exposed to brand-new medium containing 10 μM forskolin and 30 μM H-89. 0.5 ml of 6% trichloroacetic acid is added while cells are scraped off with a rubber policeman and sonicated. 2 ml of petroleum ether is added, the mixture is mixed, and the solution is centrifuged at 3000 rpm for 10 minutes to extract the trichloroacetic acid. The residue sample solution is used for analysis after aspiration of the top layer.
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Animal Protocol |
rat; mice
20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice) s.c. (Rat); i.p. (Mice) |
References |
Molecular Formula |
C20H24BRCL2N3O3S
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Molecular Weight |
519.28
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Elemental Analysis |
C, 46.26; H, 4.27; Br, 15.39; Cl, 13.65; N, 8.09; O, 6.16; S, 6.17
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CAS # |
130964-39-5
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Appearance |
Solid powder
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SMILES |
C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl
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InChi Key |
GELOGQJVGPIKAM-WTVBWJGASA-N
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InChi Code |
InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;
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Chemical Name |
N-[2-[[(E)-3-(4-bromophenyl)prop-2-enyl]amino]ethyl]isoquinoline-5-sulfonamide;dihydrochloride
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Synonyms |
H-89; H 89 HCl; H-89 Dihydrochloride; H89
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~104 mg/mL (~200.3 mM)
Water: ~6 mg/mL (~11.6 mM) Ethanol: <1 mg/mL |
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Solubility (In Vivo) |
1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.