|N-[2-[P-溴苯丙烯盐基氨基]乙基]-5-异喹啉磺酰胺二盐酸盐|CsnPharm

CAS No.: 130964-39-5

H-89 2HCl Catalog No. CSN19160

Synonyms: H-89 (hydrochloride);5-Isoquinolinesulfonamide;Protein Kinase Inhibitor H-89

H 89 2HCl is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM. It also shows weak inhibition on PKG, PKC, CK1, CK2 and others kinases.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PKA

IC50:48nM
描述PKA is a ubiquitous cellular kinase, also known as cAMP-dependent protein kinase, and it is well-established that plays an important role in regulating several functions of cell processes, including regulation of glycogen, sugar, and lipid metabolism^[1]. H-89 2HCl, as a newly synthesized isoquinolinesulfonamide, is a ATP-competitive, potent inhibitor of protein kinase A (PKA)(IC50 = 48 nM), and has weak inhibition on several other kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, respectively^[2]. H-89 2HCl has since been used extensively for evaluation of the role of PKA in the heart, osteoblasts, hepatocytes, smooth muscle cells, neuronal tissue, epithelial cells, etc^[3]. PC12D cells pretreatment with H-89 2HCl led to a dose-dependent inhibition of the forskolin-induced neurite outgrowth and protein phosphorylation. In vivo experimental method, in skinned EDL fibres of the rat, H-89 2HCl with 1-2 μM significantly slowed the repriming rate in rat skinned fibres. Moreover, rat brain ventricles following an injection with the PKA antagonist, H-89 2HCl, the body temperature is increased further due to the inhibition of TRPV1 phosphorylation^[4].
作用机制H-89 2HCl inhibit the significant modulator role of the cAMP-PKA intracellular signaling pathway mainly acting as a selective and potent inhibitor of protein kinase A (PKA).
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO	10 μM	Growth Inhibition Assay	1 h	inhibits 5-HT induced cAMP production decrease	12569069
SK-N-MC	30 μM	Function Assay	24 h	reduces the down-regulation of β1-AR by isoproterenol by 50%	11705454

动物研究

剂量

Mice: 0.05 mg/kg - 5 mg/kg^[5] (i.p.) Rat: 20 mg/kg - 200 mg/kg^[6] (s.c.)

给药途径

i.p., s.c.

动物药代数据

Animal	Rats^[6]
Dose	20 mg/kg
Administration	s.c.
MRT	6.84 h
AUC_0-inf	6951.06 ng/h/ml
T_1/2	6.78 h
T_max	4 h
C_max	436 ng/ml
AUC	6489.99 ng/h/ml

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9257 mL
- 9.6287 mL
- 19.2574 mL
- 5 mM
- 0.3851 mL
- 1.9257 mL
- 3.8515 mL
- 10 mM
- 0.1926 mL
- 0.9629 mL
- 1.9257 mL

技术信息

CAS号

130964-39-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22BrCl2N3O2S

运输

蓝冰

分子量

519.28

别名

H-89 (hydrochloride);5-Isoquinolinesulfonamide;Protein Kinase Inhibitor H-89;Protein Kinase Inhibitor;H-89 Dihydrochloride;H-89;H 89 HCl

溶解度

DMSO	195.0 mg/mL (375.5 mM)
Water	insoluble

动物实验配方

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H-89 2HCl Catalog No. CSN19160

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