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

CAS: 130964-39-5 Cat. No.: H408541 Formule: C₂₀H₂₀BrN₃O₂S.2HCl Poids moléculaire: 519.28 PubChem CID: 5702541

QUALITÉ & PURETÉ 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

Vue d’ensemble

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%

Spécifications

Synonymes

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

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

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.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Noms et identifiants

Isomères 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

Poids moléculaire

519.28

Propriétés chimiques et physiques

• Solubilité: 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)

Foire aux questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 130964-39-5, the molecular formula is C20H22BrCl2N3O2S, and the molecular weight is 519.28 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.