DMH1

製品コードS7146 バッチS714602

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C24 H20 N4 O

分子量 380.44 CAS No. 1206711-16-1
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 25 mg/mL (65.71 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
in vitro DMH1 inhibits BMP signaling with IC50 of 100 nM, and selectively inhibits the BMP-induced Smad1/5/8 activation. [1] This compound increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. [3] In addition, as a BMP inhibitor, it significantly reduces NSCLC cell growth, migration and invasion. [4]
in vivo DMH1 dorsalizes the embryonic axis without disrupting the angiogenic process in Zebrafish embryos. [1] In proepicardial explants, this compound results in the greatest inhibition of epithelial sheet migration. [2] This chemical (5 mg/kg i.p.) attenuates xenograft lung tumor growth in mice bearing A549 xenograft. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
All kinase assays are conducted by Reaction Biology Corp. In brief, this compound is tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM, using nonspecific kinase inhibitor staurosporine as control. In vitro kinase reactions are carried out in the presence of 10 μM (33P)γATP. Five kinases tested are the human BMP type-I receptor activin receptor-like kinase 2 (ALK-2/ACVR1), the human TGFβ type-I receptor activin receptor-like kinase 5 (Alk5/TGFβR1), the human VEGF type-II receptor (KDR/Flk-1/VEGFR2), the human AMP-activated protein kinase (AMPK/A1/B1/G1) and the human platelet-derived growth factor receptor-β (PDGFRβ).
細胞アッセイ 細胞株 A549 cells
濃度 ~5 μM
反応時間 48-96 hours
実験の流れ About 10,000 A549 cells per well are seeded in 96-well plates and incubated for overnight. The culture medium is then changed to fresh medium containing DMSO or DMH1 at various concentrations. The cells are then incubated for 48 hours and 96 hours before treatment termination by replacing the medium with 100 μL of 10% trichloroacetic acid in 1× PBS, followed by incubation at 4°C for at least 1 hour. Subsequently, the plates are washed with water and air dried. The plates are stained with 50 μL 0.4% sulphorhodamine assay in 1% acetic acid for 30 minutes at room temperature. Unbound dye is washed off with 1% acetic acid. After air drying and solubilization of the protein-bound dye in 10 mM Tris solution, absorbance is read in a microplate reader at 565 nm.
動物実験 動物モデル Mice bearing A549 xenograft.
投薬量 ~5 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/20020776/
  • https://pubmed.ncbi.nlm.nih.gov/21740033/
  • https://pubmed.ncbi.nlm.nih.gov/22848549/
  • https://pubmed.ncbi.nlm.nih.gov/24603907/

カスタマーフィードバック

Data from [Data independently produced by , , Anticancer Res, 2017, 37(8):4319-4327]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Human skeletal development and regeneration are shaped by functional diversity of stem cells across skeletal sites [ Cell Stem Cell, 2025, S1934-5909(25)00081-5] PubMed: 40118065
Disruption of PRC1 components RING1A and RING1B promotes angiogenesis via relieving BMP4 repression [ J Adv Res, 2025, S2090-1232(25)00553-3] PubMed: 40684938
Machine learning-based proteomics profiling of ALS identifies downregulation of RPS29 that maintains protein homeostasis and STMN2 level [ Commun Biol, 2025, 8(1):1177] PubMed: 40775435
Culture conditions differentially regulate the inflammatory niche and cellular phenotype of tracheobronchial basal stem cells [ Am J Physiol Lung Cell Mol Physiol, 2025, 328(4):L538-L553] PubMed: 39982813
Allosteric Inhibition of P-Glycoprotein-Mediated Efflux by DMH1 [ Biomedicines, 2025, 13(8)1798] PubMed: 40868055
Dual RNA sequencing of a co-culture model of Pseudomonas aeruginosa and human 2D upper airway organoids [ Sci Rep, 2025, 15(1):2222] PubMed: 39824906
Electroacupuncture Preconditioning Ameliorates the Ischemic Microenvironment to Improve Long-Term Potentiation in Chronic Cerebral Hypoperfusion Rats With MGE Neural Progenitor Transplantation [ Neural Plast, 2025, 2025:9933756] PubMed: 40969839
Fungal melanin suppresses airway epithelial chemokine secretion through blockade of calcium fluxing [ Nat Commun, 2024, 15(1):5817] PubMed: 38987270
A TBK1 variant causes autophagolysosomal and motoneuron pathology without neuroinflammation in mice [ J Exp Med, 2024, 221(5)e20221190] PubMed: 38517332
Novel role of bone morphogenetic protein 9 in innate host responses to HCMV infection [ EMBO Rep, 2024, 25(3):1106-1129] PubMed: 38308064

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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