产品说明书

DMH-1

Print
Chemical Structure| 1206711-16-1 同义名 : BMP Inhibitor II;VU036482;DorsoMorphin Homolog 1
CAS号 : 1206711-16-1
货号 : A590459
分子式 : C24H20N4O
纯度 : 99%+
分子量 : 380.442
MDL号 : MFCD18384963
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 10 mg/mL(26.29 mM)，配合低频超声，并水浴加热至45℃助溶，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
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

生物活性
靶点

  • ALK2

    ALK2, IC50:107.9 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL
参考文献

[1]Hao J, Ho JN, et al. In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol. 2010 Feb 19;5(2):245-53.

[2]Williams E, Bullock AN, et al. Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2. Bone. 2018 Apr;109:251-258.

[3]Owens P, Pickup MW, et al. Inhibition of BMP signaling suppresses metastasis in mammary cancer. Oncogene. 2015 May 7;34(19):2437-49.

[4]Neely MD, Litt MJ, et al. DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction. ACS Chem Neurosci. 2012 Jun 20;3(6):482-91.

[5]Ao A, Hao J, et al. DMH1, a novel BMP small molecule inhibitor, increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. PLoS One. 2012;7(7):e41627.

[6]Williams E, Bullock AN, et al. Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2. Bon