H 89 2HCl

Name: H 89 2HCl
SKU: H408541
Availability: InStock

H 89 2HCl

CAS: 130964-39-5 货号: H408541 分子式: C₂₀H₂₀BrN₃O₂S.2HCl 分子量: 519.28 PubChem CID: 5702541

概述规格名称和识别符高级数据质检证书(CoA,COO,BSE/TSE 和分析图谱) 化学和物理性质此产品的引用文献技术文档和文章溶液计算器常见问题

概述

H 89 2HCl是一种有效的PKA抑制剂，Ki为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC， MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。

应用：

H-89二盐酸盐水合物抑制蛋白激酶A，用于Leydig细胞、原代颅骨成骨细胞（pOB）、大鼠颗粒细胞系（LH-15细胞）[3] 和人脐静脉内皮细胞（HUVEC）。

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%

规格

英文别名

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

规格或纯度

10mM in DMSO

英文名称

H 89 2HCl

生化机理

H 89 2HCl 是一种强效的 PKA 抑制剂，在无细胞试验中的_Ki值为 48 nM，对 PKA 的选择性是 PKG 的 10 倍，是 PKC、MLCK、钙调素激酶 II 和酪蛋白激酶 I/II 的 500 倍。H 89 2HCl 可诱导自噬。

储存条件

-80℃储存

运输条件

特低温运输

名称和识别符

分子类型

小分子

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

分子量

519.28

高级数据

化学和物理性质

溶解性

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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批号(Lot Number)	证书类型	货号
C2314030	分析证书	H408541

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