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Dorsomorphin {[allProObj[0].p_purity_real_show]}

货号:A137399 同义名: Compound C

Dorsomorphin 是一种选择性、ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下,Ki 为 109 nM),选择性抑制 BMP I 型受体 ALK2ALK3ALK6,并可逆转 Urolithin A导致的自噬激活和抗炎作用。

Dorsomorphin 化学结构 CAS号:866405-64-3
Dorsomorphin 化学结构
CAS号:866405-64-3
Dorsomorphin 3D分子结构
CAS号:866405-64-3
Dorsomorphin 化学结构 CAS号:866405-64-3
Dorsomorphin 3D分子结构 CAS号:866405-64-3
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Dorsomorphin 纯度/质量文件 产品仅供科研

货号:A137399 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AMPK 其他靶点 纯度
WZ4003 ++++

NUAK2, IC50: 100 nM

NUAK1, IC50: 20 nM

98+%
Dorsomorphin ++

AMPK, Ki: 109 nM

99%
HTH-01-015 +++

NUAK1 , IC50: 100 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。

Dorsomorphin 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].

Dorsomorphin 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

Dorsomorphin 动物研究

Dose Mice: 3 mg/kg - 12 mg/kg[3] (i.p.) Rat: 0.2 mg/kg[4] (i.v.)
Administration i.p., i.v.

Dorsomorphin 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.

Dorsomorphin 实验方案

计算器
存储液制备 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

Dorsomorphin 技术信息

CAS号866405-64-3
分子式C24H25N5O
分子量 399.488
别名 Compound C
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

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

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