产品说明书

Dorsomorphin

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Chemical Structure| 866405-64-3 同义名 : Compound C
CAS号 : 866405-64-3
货号 : A137399
分子式 : C24H25N5O
纯度 : 99%
分子量 : 399.488
MDL号 : MFCD08705402
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(87.61 mM),配合低频超声,并调节pH至2,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

1M HCl: 50 mg/mL(125.16 mM),配合低频超声,并调节pH至1

动物实验配方:

IP 2% DMSO+water 0.04 mg/mL clear

PO 0.5% CMC-Na 55 mg/mL suspension

生物活性
靶点
  • AMPK

    AMPK, Ki:109 nM

描述 Dorsomorphin, known as compound C, is a reversible selective ATP-competitive inhibitor of AMPK with Ki of 109 nM. Dorsomorphin can also inhibit the bone morphogenic protein (BMP) signaling and do not effect the expression of several structurally related kinases including ZAPK, SYK, PKCq, PKA, and JAK3[3]. In addition, dorsomorphin could stimulate the oxidation of long chain fatty acids independently in adipocytes by increasing carnitine palmitoyltransferase-1 (CPT1) activity[4] and remarkly reduce the adipogenic Differentiation of 3T3-L1 cells at 10 μM[5]. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway[6]. In vivo, dorsomorphin induces dorsalization in zebrafish embryos and the differentiation of osteoblast[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
mouse C2C12 cells 4 μM Function assay Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry 18026094
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL

参考文献

[1](6):100-6. Russian.

[2]281(36):25956-64.

[3]Kutiakov MG. Rezul'taty rezektsii zheludka po povodu iazvennoĭ bolezni [Results of stomach resection for peptic ulcer]. Khirurgiia (Mosk). 1975 Jun;(6):100-6. Russian.

[4]Gaidhu MP, Fediuc S, Ceddia RB. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside-induced AMP-activated protein kinase phosphorylation inhibits basal and insulin-stimulated glucose uptake, lipid synthesis, and fatty acid oxidation in isolated rat adipocytes. J Biol Chem. 2006 Sep 8;281(36):25956-64.

[5]Gao Y, Zhou Y, Xu A, Wu D. Effects of an AMP-activated protein kinase inhibitor, compound C, on adipogenic differentiation of 3T3-L1 cells. Biol Pharm Bull. 2008 Sep;31(9):1716-22.