H 89 2HCl - 10mM in DMSO , CAS No.130964-39-5

CAS: 130964-39-5 Cat. No.: H408541 Formula: C₂₀H₂₀BrN₃O₂S.2HCl Peso molecolare: 519.28 PubChem CID: 5702541

GRADE & PURITY 10mM in DMSO

Synonyms

(E)-N-(2-(4-bromocinnamylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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 K_i 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%

Specifications

Sinonimi

(E)-N-(2-(4-bromocinnamylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

H 89 2HCl is a potent PKA inhibitor with K_i 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. H 89 2HCl induces autophagy.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Isomeri 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
• Peso molecolare: 519.28

Proprietà chimiche e fisiche

• Solubilità: 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)

Riferimenti

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]