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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 |
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分子量 | 380.44 | CAS No. | 1206711-16-1 | |
Solubility (25°C)* | 体外 | DMSO | 12 mg/mL warmed with 50ºC water bath (31.54 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
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. |
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in vitro | DMH1 inhibits BMP signaling with IC50 of 100 nM, and selectively inhibits the BMP-induced Smad1/5/8 activation. [1] DMH1 increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells. [3] In addition, DMH1 as a BMP inhibitor, 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, DMH1 results in the greatest inhibition of epithelial sheet migration. [2] DMH1 (5 mg/kg i.p.)attenuates xenograft lung tumor growth in mice bearing A549 xenograft. [4] |
キナーゼアッセイ | Kinase assay | |
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All kinase assays are conducted by Reaction Biology Corp. In brief, compounds are 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. |
Data from [Data independently produced by , , Anticancer Res, 2017, 37(8):4319-4327]
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 |
The use of a SOX10 reporter toward ameliorating oligodendrocyte lineage differentiation from human induced pluripotent stem cells [ Glia, 2024, 72(6):1165-1182] | PubMed: 38497409 |
The MORC2 p.S87L mutation reduces proliferation of pluripotent stem cells derived from a patient with the spinal muscular atrophy-like phenotype by inhibiting proliferation-related signaling pathways [ Neural Regen Res, 2024, 19(1):205-211] | PubMed: 37488868 |
Homozygous ALS-linked mutations in TARDBP/TDP-43 lead to hypoactivity and synaptic abnormalities in human iPSC-derived motor neurons [ iScience, 2024, 27(3):109166] | PubMed: 38433895 |
Chronic Oxidative Stress and Stress Granule Formation in UBQLN2 ALS Neurons: Insights into Neuronal Degeneration and Potential Therapeutic Targets [ Int J Mol Sci, 2024, 25(24)13448] | PubMed: 39769213 |
Culture Conditions Differentially Regulate the Inflammatory Niche and Cellular Phenotype of Tracheo-Bronchial Basal Stem Cells [ bioRxiv, 2024, 2024.09.04.611264] | PubMed: 39282256 |
Single-cell analysis of human airway epithelium identifies cell type-specific responses to Aspergillus and Coccidioides [ bioRxiv, 2024, 2024.09.09.612147] | PubMed: 39314271 |
Generation of self-renewing neuromesodermal progenitors with neuronal and skeletal muscle bipotential from human embryonic stem cells [ Cell Rep Methods, 2024, 4(11):100897] | PubMed: 39515335 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。