Dorsomorphin (Compound C)

製品コードS7840 バッチS784005

化学情報

	Synonyms	BML-275,Compound C	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₅N₅O
	分子量	399.49	CAS No.	866405-64-3
Solubility (25°C)*	体外	DMSO	5 mg/mL (12.51 mM)
		Ethanol	2 mg/mL (5.0 mM)
		Water	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	Dorsomorphin は、無細胞アッセイで K_i が 109 nM の強力で可逆的、選択的な AMPK 阻害剤であり、ZAPK、SYK、PKCθ、PKA、JAK3 などの構造的に関連するいくつかのキナーゼに対して有意な阻害を示しません。Dorsomorphin は、BMP タイプ I 受容体 ALK2、ALK3、ALK6 を選択的に阻害します。Dorsomorphin は、特定の細胞分化の促進やがん細胞株のオートファジー誘導に使用されます。動物実験には、水溶性の S7306 Dorsomorphin (Compound C) 2HCl が推奨されます。
in vitro	Dorsomorphin inhibits ACC inactivation by either AICAR, and also attenuates AICAR’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. Inhibition of AMPK activity by this compound almost completely inhibits autophagic proteolysis in HT-29 cells. In addition, this chemical selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation.
in vivo	Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. This compound (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats.

製品説明

Dorsomorphin は、無細胞アッセイで K_i が 109 nM の強力で可逆的、選択的な AMPK 阻害剤であり、ZAPK、SYK、PKCθ、PKA、JAK3 などの構造的に関連するいくつかのキナーゼに対して有意な阻害を示しません。Dorsomorphin は、BMP タイプ I 受容体 ALK2、ALK3、ALK6 を選択的に阻害します。Dorsomorphin は、特定の細胞分化の促進やがん細胞株のオートファジー誘導に使用されます。動物実験には、水溶性の S7306 Dorsomorphin (Compound C) 2HCl が推奨されます。

in vitro

Dorsomorphin inhibits ACC inactivation by either AICAR, and also attenuates AICAR’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes.

Inhibition of AMPK activity by this compound almost completely inhibits autophagic proteolysis in HT-29 cells.

In addition, this chemical selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation.

in vivo

Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice.

This compound (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats.

プロトコル(参考用のみ)

キナーゼアッセイ	AMPK partial purification and in vitro kinase assay.
キナーゼアッセイ	Liver AMPK is partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contains 100 μM AMP, 100 μM ATP (0.5 μCi ³³P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES, pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl₂, 0.025% BSA, and 0.8 mM DTT). The reaction is initiated with addition of the enzyme. After 30-minute incubation at 30°C, the reaction is stopped by addition of 80 μl 1% H₃PO₄. Aliquots (100 μl) are transferred to 96-well MultiScreen plates. The plate is washed three times with 1% H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with this compound are fit to the following equation for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (K_m + S)/[S + K_m × (1 + I/K_i)], where Vi is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, K_m is the Michaelis constant for ATP, I is the inhibitor (this chemical) concentration, and K_i is the dissociation constant for this compound.
細胞アッセイ	細胞株	Cell-free assays
	濃度	109 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Iron-replete mice
	投薬量	~10 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/11602624/
https://pubmed.ncbi.nlm.nih.gov/16990266/
https://pubmed.ncbi.nlm.nih.gov/18026094/

https://pubmed.ncbi.nlm.nih.gov/21764059/

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カスタマーフィードバック

: , , J Cell Physiol, 2017, 232(7):1893-1906

: , , Clin Exp Pharmacol Physiol, 2016, 43(1):125-34.

: Data from [Data independently produced by , , Oncotarget, 2016, 6(41):43605-19.]

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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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