H-89 DIHYDROCHLORIDE HYDRATE
H 89 2HCl
CAS: 130964-39-5
Molecular Formula: C20H20BrN3O2S.2ClH.H2O
H-89 DIHYDROCHLORIDE HYDRATE - Names and Identifiers
H-89 DIHYDROCHLORIDE HYDRATE - Physico-chemical Properties
| Molecular Formula | C20H20BrN3O2S.2ClH.H2O |
| Molar Mass | 537.304 |
| Melting Point | 195-200°C |
| Solubility | DMSO 104 mg/mL Water 6 mg/mL Ethanol <1 mg/mL |
| Appearance | White-like powder |
| Color | off-white |
| Storage Condition | Inert atmosphere,2-8°C |
| MDL | MFCD11045926 |
| In vitro study | H89 2HCl is A potent PKA (cAMP-dependent) protein kinase A inhibitor with A K I value of 48 nM and A selectivity 10-fold higher than PKG, compared to PKC,MLCK, calmodulin kinase II and casein kinase I / II are over 500-fold higher. Pretreatment of cells with H-89 (30 μm) for 1 hour prior to addition of forskolin significantly inhibited forskolin-induced protein phosphorylation in a dose-dependent manner. H89 also inhibited several other kinases with IC50 values of 80, 120,135,270,2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, pkbα and MAPKAP-K1b, respectively. H89 on several cellular receptors and ion channels, including Kv1.3 K |
| In vivo study | H89 leads to significant changes in protein phosphorylation, of which the greatest changes in phosphorylation are Levulose -1, 6-bisphosphatase, isomeric nuclear ribonucleoprotein (hnRNP),NSFL1 cofactor P47, all of these have a potential regulatory link with cAMP/PKA. |
H-89 DIHYDROCHLORIDE HYDRATE - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
H-89 DIHYDROCHLORIDE HYDRATE - Introduction
H 89 2HCl is a potent PKA inhibitor with a Ki of 48 nM, acting on PKA is 10 times more selective than acting on PKG and 500 times more selective than acting on PKC, MLCK, calmodulin kinase II and casein I/II.
Last Update：2022-10-16 17:41:24
H-89 DIHYDROCHLORIDE HYDRATE - Reference Information
| traits | H-89 dihydrochloride Chinese alias N-[2-[P-bromophenylpropenylamino] ethyl]-5-isoquinoline sulfonamide dihydrochloride, storage condition: 2-8°C, gray powder. Its character map is as follows: |
| preparation | weigh 5-isoquinoline sulfonyl chloride and P-bromobenzene propylene chloride to dissolve in 180mL tetrahydrofuran. after dissolving, slowly add the solution to 200mL ethylenediamine solution under the condition of ice water bath, and immediately precipitate solid. after adding, continue to stir for 4 hours at 35 ℃, and detect the reaction progress by thin layer chromatography. After the reaction is completed and the reaction solution is cooled, 400mL of ice water is added to the reaction to completely precipitate the product and filter to obtain a light yellow solid. After drying, dissolve with anhydrous ethanol, add dilute hydrochloric acid dropwise, solid precipitation, acetone recrystallizes to obtain white solid H-89 dihydrochloride. |
| biological activity | H 89 2HCl is an effective PKA inhibitor. in cell-free test, Ki is 48 nM, which is 10 times more selective than PKA and 500 times more selective than PKC,MLCK, calmodulin kinase II and casein excitation I/II. H 89 2HCl induces autophagy. |
| target | TargetValue PKA (Cell-Free Assay) 48 nM(Ki) S6K1 (Cell-Free Assay) 80 nM PKG (Cell-Free Assay) 0.48 μ M(Ki) |
| Target | Value |
| PKA (Cell-free assay) | 48 nM(Ki) |
| S6K1 (Cell-free assay) | 80 nM |
| PKG (Cell-free assay) | 0.48 μM(Ki) |
| in vitro study | H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with a K I value of 48 nM and a selectivity of 10 times higher than PKG and more than 500 times higher than PKC,MLCK, calmodulin kinase II and casein kinase I/II. Pretreatment of cells with H-89 (30 μM) for 1 hour before forskolin addition will significantly inhibit forskolin-induced protein phosphorylation in a dose-dependent manner. H89 also inhibits several other kinases, with IC50 values of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKB α and MAPKAP-K1b, respectively. H89 for some cell receptors and ion channels, including Kv1.3 K |
| In vivo research | H89 leads to obvious changes in protein phosphorylation, of which the largest changes in phosphorylation are levoxyl-1, 6-diphosphatase, isomeric ribonucleoprotein (hnRNP),NSFL1 cofactor P47, all of which have potential regulatory links with cAMP/PKA. |
Last Update：2024-04-09 19:05:04
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View History
H-89 DIHYDROCHLORIDE HYDRATE
(3R)-3-[[(1,1-二甲基乙基)二甲基硅烷基]氧基]-5-氧代-1-环戊烯-1-庚酸甲酯
BENZOIC ACID, 4-[[[(3-CHLORO-4-ETHOXYBENZOYL)AMINO]THIOXOMETHYL]AMINO]-
L-6-OXO-PIPECOLINIC ACID
(3R)-3-[[(1,1-二甲基乙基)二甲基硅烷基]氧基]-5-氧代-1-环戊烯-1-庚酸甲酯
BENZOIC ACID, 4-[[[(3-CHLORO-4-ETHOXYBENZOYL)AMINO]THIOXOMETHYL]AMINO]-
L-6-OXO-PIPECOLINIC ACID