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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
H 89 2HCl is a potentPKAinhibitor withKiof 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. H 89 2HCl inducesautophagy.
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. 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. H89 also has activity at some cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR.
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. H-89 (0.5, 1, 5 mg/kg) significantly attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice.
Cell Data
cell lines:
Concentrations:~30 μM
Incubation Time:1 h
Powder Purity:≥99%
| Isomeric SMILES | C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl |
|---|---|
| PubChem CID | 5702541 |
| Molecular Weight | 519.28 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | Solubility (25°C) In vitro Water: 49 mg/mL (199.37 mM); DMSO: 24 mg/mL (97.65 mM); Ethanol: 10 mg/mL (40.68 mM); |
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| 1. Zhao Huang, Li Zhou, Jiufei Duan, Siyuan Qin, Jingwen Jiang, Haining Chen, Kui Wang, Rui Liu, Minlan Yuan, Xiangdong Tang, Edouard C. Nice, Yuquan Wei, Wei Zhang, Canhua Huang. (2024) Oxidative Stress Promotes Liver Cancer Metastasis via RNF25-Mediated E-Cadherin Protein Degradation. Advanced Science, [PMID:38286671] [10.1002/advs.202306929] |