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CAS No.: 1206711-16-1

DMH-1 Catalog No. CSN17559

Synonyms: BMP Inhibitor II;DorsoMorphin Homolog 1;VU036482

DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/< 5 nM for ALK1/2/3 respectively and inactive on ALK5, BMPR2, AMPK and VEGFR2.

规格	价格	促销价格	库存	数量

400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ALK1

IC50:27nM ALK2

IC50:107.9nM ALK3

IC50:5nM
描述BMPs (Bone morphogenetic proteins) represent the largest subgroup in the TGFβ family of extracellular ligands. Their signaling transduction requires the interaction with the type I and type II transmembrane receptor kinase. Type I receptors, such as ALK1/ACVRL1, ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B all participate in BMP signaling and phosphorylate SMAD1/5/ 8 of SMAD family transcription factors^[2]. DMH-1 is a selective inhibitor of BMP type I receptors with IC50 values of 107.9 nM for ALK2 and with no activity on ALK5, AMPK, VEGFR2 or PDGFRβ (measured by in vitro kinase assays). DMH1 on concentration of 1-20 μM blocked BMP4-induced Smad 1/5/8 phosphorylation dose-dependently in HEK293 cells. In contrast, DMH1 had no effect on BMP4-induced p38 MAPK phosphorylation or Activin A-induced Smad2 phosphorylation^[1]. Mice expressing MMTV.PyVmT, with six-week pumps containing 7 mg DMH1, showed reduced lung metastasis and the tumors were less proliferative and more apoptotic compared with the control group^[3]. DMH1 is also used in cell differentiation or reprogramming, for example: 1.Combined with SB431542, DMH1 can induce neuralization of hiPSCs^[4]. 2. DMH1 can increase cardiomyocyte progenitors and promote cardiac differentiation in mouse embryonic stem cells^[5].
作用机制DMH-1 targets to the ATP-binding pocket located within the intracellular kinase domain of the receptors.^[6]
动物研究
剂量
Mice^[7] (i.p.): 5 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Mice^[7] (i.p.): 5 mg/kg
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6285 mL
- 13.1427 mL
- 26.2854 mL
- 5 mM
- 0.5257 mL
- 2.6285 mL
- 5.2571 mL
- 10 mM
- 0.2629 mL
- 1.3143 mL
- 2.6285 mL

技术信息

CAS号

1206711-16-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H20N4O

运输

蓝冰

分子量

380.44

别名

BMP Inhibitor II;DorsoMorphin Homolog 1;VU036482

溶解度

DMSO	33.0 mg/mL (86.7 mM) warming
Water	insoluble

动物实验配方

IP	3% DMSO+2% Tween80+40% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	40 mg/mL	suspension

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靶点	Description	IC50
ALK1		IC50:27nM
ALK2		IC50:107.9nM
ALK3		IC50:5nM

DMH-1 Catalog No. CSN17559

靶点选择性

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