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Merck
CN

P5499

Sigma-Aldrich

Dorsomorphin

≥98% (HPLC), powder, AMPK inhibitor

别名:

6-[4-(2-哌啶基-1-乙氧基)苯基]-3-吡啶基-4-吡唑并[1,5-a]嘧啶, AMPK抑制剂, Compound C, Dorsomorphin

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About This Item

经验公式(希尔记法):
C24H25N5O
分子量:
399.49
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.77

product name

Dorsomorphin, ≥98% (HPLC)

质量水平

检测方案

≥98% (HPLC)

形式

powder

储存条件

protect from light

颜色

white to beige

溶解性

DMSO: >2 mg/mL (warmed)

储存温度

2-8°C

SMILES字符串

C1CCN(CC1)CCOc2ccc(cc2)-c3cnc4c(cnn4c3)-c5ccncc5

InChI

1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2

InChI key

XHBVYDAKJHETMP-UHFFFAOYSA-N

一般描述

Dorsomorphin got its name due to its ability to induce dorsoventral patterning abnormalities in zebrafish, a characteristic trait of BMP-pathway mutant embryos. Structurally, dorsomorphin is identical to compound C. Dorsomorphin induces stem cell differentiation, suggesting potential therapeutic implications for fibrodysplasia ossificans progressiva (FOP), a progressive muscle and bone disease. Besides its BMP signaling inhibition, dorsomorphin also hinders the vascular endothelial growth factor (VEGF) type 2 receptor (FLK1/KDR) and disrupts angiogenesis during zebrafish development.

应用

Dorsomorphin可用于:
  • 用作磷酸腺苷激活蛋白激酶(APK)的抑制剂,寻找白藜芦醇对3T3-L1(小鼠脂肪细胞系)细胞中脂质移动的影响
  • 用作AMPK抑制剂,指示AMPK/mTOR(哺乳动物雷帕霉素靶蛋白)通路参与LRG(利拉鲁肽)诱导的自噬
  • 在诱导步骤中,利用胚胎干细胞(ES)培养基,将弗里德的共济失调(FRDA)和诱导多能干细胞(iPSC)向经球和神经元体外分化

生化/生理作用

Dorsomorphin是骨形态生成蛋白(BMP)信号传导的选择性抑制剂。已有研究发现它能够抑制胚胎形成所需的BMP信号,并显著促进人多能干细胞(hPSC)的神经分化。 Dorsomorphin还可作为AMPK(AMP活化蛋白激酶)的有效的、选择性、可逆性和ATP竞争性抑制剂;当存在5μM的ATP且不存在AMP时,Ki = 109 nM)。

特点和优势

《受体分类和信号转导》手册的 AMPK 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处
该化合物是激酶磷酸酶生物学研究推荐产品。点击此处 ,查看更多激酶磷酸酶生物学精选产品。想要了解有关生物活性小分子在其他研究领域应用的更多信息,请访问 sigma.com/discover-bsm

WGK

WGK 3

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


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Does bone morphogenetic protein 2 (BMP2) regulate connexin43 (Cx43) and modulate cell-cell communication in luteinized human granulosa cells? BMP2 decreases gap junction intercellular communication (GJIC) of luteinized human granulosa cells by down-regulating Cx43 expression through an activin receptor-like kinase (ALK)2/ALK3-mediated
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Molecular medicine reports, 13(2), 1577-1585 (2016-01-01)
Hypoxia induces pulmonary vasoconstriction and reconstruction in the pulmonary arteries and pulmonary veins (PVs), and elevation of intracellular calcium concentration ([Ca2+]i) is a primary factor of these processes. In the present study, the role of transient receptor potential cation channels
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Development (Cambridge, England), 138(1), 97-106 (2010-12-01)
In zebrafish, Hedgehog-induced Engrailed expression defines a muscle fibre population that includes both slow and fast fibre types and exhibits an organisational role on myotome and surrounding tissues, such as motoneurons and lateral line. This Engrailed-positive population is restricted in

商品

The AMP-activated protein kinase (AMPK) acts as a sensor of cellular energy status. AMPK exists as heterotrimeric complexes comprising a catalytic α subunit and regulatory β and γ subunits.

Naive pluripotent stem cells cultured in vitro using specialized media and inhibitors mimic "ground-state" cells from blastocysts.

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

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