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 | |
Additional Infomation |
N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide dihydrochloride is a hydrochloride salt prepared from N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide and two equivalents of hydrogen chloride. It has a role as an EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor. It contains a N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide(2+).
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Molecular Formula |
C20H24BRCL2N3O3S
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Molecular Weight |
519.28
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Exact Mass |
516.9993
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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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Related CAS # |
H-89;127243-85-0
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PubChem CID |
5702541
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Appearance |
White to light yellow solid powder
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Melting Point |
195-200ºC
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tPSA |
79.5Ų
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
Solubility in Formulation 1: 5 mg/mL (9.63 mM) in 10% DMSO + 90% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.30 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (5.30 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: ≥ 0.55 mg/mL (1.06 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 8: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
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.