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

CAS: 130964-39-5 Cat. No.: H408541 分子式: C₂₀H₂₀BrN₃O₂S.2HCl 分子量: 519.28 PubChem CID: 5702541

グレード＆純度 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

概要

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%

仕様

同義語

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

名前と識別子

異性体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

分子量

519.28

化学的性質と物理的性質

• 溶解度: 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)

よくある質問

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.