H-89 Dihydrochloride

製品コードS1582 バッチS158201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₀BrN₃O₂S.2HCl
	分子量	519.28	CAS No.	130964-39-5
Solubility (25°C)*	体外	DMSO	104 mg/mL (200.27 mM)
		Water	6 mg/mL (11.55 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	H 89 2HClは、無細胞アッセイにおいて48 nMのK_iを有する強力なPKA阻害剤であり、PKGに対してPKAより10倍、PKC、MLCK、カルモジュリンキナーゼII、およびカゼインキナーゼI/IIより500倍高い選択性を示します。H 89 2HClはautophagyを誘導します。
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 this compound (30 μM) 1 h before the addition of forskolin markedly inhibits the forskolin-induced protein phosphorylation in a dose-dependent manner. This compound 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. It 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.

プロトコル(参考用のみ)

キナーゼアッセイ	PKA enzyme activity
キナーゼアッセイ	cAMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HC1 (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cAMP or absence of cAMP, 3.3-20 μM [γ-³²P]ATP (4 × 10⁵ cpm), 0.5 μg of the enzyme, 100 μg of histone H2B, and each compound, as indicated.
細胞アッセイ	細胞株	PC12D
	濃度	~30 μM
	反応時間	1 h
	実験の流れ	Levels of intracellular cAMP are determined. After 48 h in culture, PC12D cells are cultured in test medium containing 30 μM H-89 for 1 h and then exposed to fresh medium that contained both 10 μM forskolin and 30 μM this compound. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5 ml of 6% trichloroacetic acid. To extract trichloroacetic acid, 2 ml of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination.
動物実験	動物モデル	rat; mice
	投薬量	20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice)
	投与方法	s.c. (Rat); i.p. (Mice)

参考

https://pubmed.ncbi.nlm.nih.gov/2156866/
https://pubmed.ncbi.nlm.nih.gov/10998351/
https://pubmed.ncbi.nlm.nih.gov/17214602/

https://pubmed.ncbi.nlm.nih.gov/18523239/
https://pubmed.ncbi.nlm.nih.gov/16687476/

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カスタマーフィードバック

: Data from [Data independently produced by , , J Cell Physiol, 2015, 230: 2233-2239]

: Data from [Data independently produced by , , Eur J Pharm Sci, 2015, 70C: 82-91 ]

: Data from [Data independently produced by , , Sci Rep, 2016, 6:26835.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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