H-89 2HCl | H-89 (hydrochloride) | PKA Inhibitor | AmBeed-信号通路专用抑制剂

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H-89 2HCl {[allProObj[0].p_purity_real_show]}

货号：A171227 同义名： H-89 (hydrochloride);Protein Kinase Inhibitor H-89

H-89 2HCl是一种高效且选择性的蛋白激酶A（PKA）抑制剂，IC50为48 nM，对PKG、PKC和酪蛋白激酶的抑制作用较弱。

H-89 2HCl 化学结构
CAS号：130964-39-5

H-89 2HCl 3D分子结构
CAS号：130964-39-5

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H-89 2HCl 纯度/质量文件产品仅供科研

货号：A171227 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PKC 亚型比较
PKA 亚型比较
转化生长因子-β 亚型比较
Casein Kinase 亚型比较

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									EGFR,PKA	95%
Dequalinium Chloride											99%+
Quercetin	✔									Sirtuin,Src	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 μM			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	PKA ↓ ↑	其他靶点	纯度
Daphnetin	+ PKA, IC50: 9.33 μM	EGFR,PKC	95%
AT13148	++++ PKA, IC50: 3 nM		98+%
A-674563 HCl	+++ PKA, Ki: 16 nM		98%
H-89 2HCl	++ PKA, Ki: 48 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	CK1 ↓ ↑	CK2 ↓ ↑	其他靶点	纯度
PF-670462 2HCl	++++ CK1δ, IC50: 13 nM CK1ε, IC50: 90 nM			99%+
D4476	++ CK1δ, IC50: 300 nM CK1 from Schizosaccharomyces pombe, IC50: 200 nM			98%
SR-3029	+++ CK1δ, IC50: 44 nM CK1ε, IC50: 260 nM			99%+
IWP-2	+++ ^M82FCK1δ, IC50: 40 nM		Wnt	98%
LY364947	++ CK1δ, IC50: 0.22 μM			98%
TA-01	++++ CK1δ, IC50: 6.8 nM CK1ε, IC50: 6.4 nM		p38 MAPK	99%+
IC261	+ CK1, IC50: 16 μM			98%
PF-4800567	+++ casein kinase 1 delta, IC50: 711 nM casein kinase 1 epsilon, IC50: 32 nM			99%+
CK1-IN-1	++++ CK1δ, IC50: 15 nM CK1ε, IC50: 16 nM			98%
Longdaysin	+ CKIα, IC50: 5.6 μM CKIδ, IC50: 8.8 μM			99%+
Silmitasertib		++++ CK2, IC50: 1 nM		99%+
Ellagic acid (hydrate)		+++ CK2, IC50: 0.04 μM	PKA	95+%
DMAT		+++ CK2, Ki: ~40 nM		98%
Hematein		++ CK2, IC50: 0.55 μM		98+%
Silmitasertib sodium salt		++++ CK2α', IC50: 1 nM CK2α, IC50: 1 nM		99%+
LY294002		+++ CK2, IC50: 98 nM		99%+
A-3 HCl	+ CK1, Ki: 80 μM	++ CK2, Ki: 5.1 μM	PKC,PKA,MLCK	98+%
TBB	+ CK1, Ki: 47 μM	++ CK2, Ki: 0.4 μM		98%
TTP 22		++ CK2, IC50: 100 nM		98%+
DRB		✔		99%+
BioE-1115		+ CK2α, IC50: 10 μM		99%+
(E/Z)-GO289		++++ CK2, IC50: 7 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

H-89 2HCl 生物活性

靶点	PKA PKA, Ki:48 nM
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).

H-89 2HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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

H-89 2HCl 动物研究

Dose

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

Administration

i.p., s.c.

Pharmacokinetics

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

H-89 2HCl 参考文献

[1]Dolan S, Nolan AM. Biphasic modulation of nociceptive processing by the cyclic AMP-protein kinase A signalling pathway in sheep spinal cord. Neurosci Lett. 2001;309(3):157-60.

[2]Chijiwa T, Mishima A, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol Chem. 1990;265(9):5267-72.

[3]Lochner A, Moolman JA. The many faces of H89: a review. Cardiovasc Drug Rev. 2006;24(3-4):261-74.

[4]Bao D, Zhao W, et al. H89 dihydrochloride hydrate and calphostin C lower the body temperature through TRPV1. Mol Med Rep. 2018;17(1):1599-1608.

[5]Seyedi SY, Salehi F, et al. Dual effect of cAMP agonist on ameliorative function of PKA inhibitor in morphine-dependent mice. Fundam Clin Pharmacol. 2014 Aug;28(4):445-54.

[6]Davis MA, Hinerfeld D, et al. Proteomic analysis of rat liver phosphoproteins after treatment with protein kinase inhibitor H89 (N-(2-[p-bromocinnamylamino-]ethyl)-5-isoquinolinesulfonamide). J Pharmacol Exp Ther. 2006 Aug;318(2):589-95. Epub 2006 May 10.

H-89 2HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.63mL

1.93mL

0.96mL

19.26mL

3.85mL

1.93mL

H-89 2HCl 技术信息

CAS号	130964-39-5
分子式	C₂₀H₂₂BrCl₂N₃O₂S
分子量	519.283

别名	H-89 (hydrochloride);Protein Kinase Inhibitor H-89;5-Isoquinolinesulfonamide;H-89 dihydrochloride
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(202.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 5 mg/mL(9.63 mM)，配合低频超声，并水浴加热至45℃助溶

动物实验配方

H-89 2HCl {[allProObj[0].p_purity_real_show]}

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H-89 2HCl 技术信息

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