受注:045-509-1970 |
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Synonyms | BML-275 2HCl,Compound C 2HCl | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H25N5O.2HCl |
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分子量 | 472.41 | CAS No. | 1219168-18-9 | ||||
Solubility (25°C)* | 体外 | Water | 94 mg/mL (198.97 mM) | ||||
DMSO | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line. |
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in vitro | Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] In addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3] |
in vivo | Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4] |
キナーゼアッセイ | AMPK partial purification and in vitro kinase assay. | |
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Liver AMPK is partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contains 100 μM AMP, 100 μM ATP (0.5 μCi 33P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES, pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl2, 0.025% BSA, and 0.8 mM DTT). The reaction is initiated with addition of the enzyme. After 30-minute incubation at 30°C, the reaction is stopped by addition of 80 μl 1% H3PO4. Aliquots (100 μl) are transferred to 96-well MultiScreen plates. The plate is washed three times with 1% H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with compound C — (6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine — are fit to the following equation for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (Km + S)/[S + Km × (1 + I/Ki)], where Vi is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, Km is the Michaelis constant for ATP, I is the inhibitor (compound C) concentration, and Ki is the dissociation constant for compound C. | ||
細胞アッセイ | 細胞株 | NIH3T3 cells |
濃度 | 10 μM | |
反応時間 | 3 days | |
実験の流れ | Cells were treated with hydrogen peroxide and incubated in complete medium with or without treatment with the AMPK activators metformin (10 μM), AICAR (10 μM), alone or plus AMPK inhibitor Compound C (CC, 10 μM) for 3 days. |
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動物実験 | 動物モデル | Iron-replete mice |
投薬量 | ~10 mg/kg | |
投与方法 | i.v. |
, , Mol Brain, 2015 ,8:20.
, , FEBS Lett, 2015, 589(15):1847-54.
, , FEBS Letters, 2015, 1847-1854.
Automated, High-Throughput Phenotypic Screening and Analysis Platform to Study Pre- and Post-Implantation Morphogenesis in Stem Cell-Derived Embryo-Like Structures [ Adv Sci (Weinh), 2024, 11(4):e2304987] | PubMed: 37991133 |
HiHo-AID2: boosting homozygous knock-in efficiency enables robust generation of human auxin-inducible degron cells [ Genome Biol, 2024, 25(1):58] | PubMed: 38409044 |
Molecular mechanism underlying miR-204-5p regulation of adipose-derived stem cells differentiation into cells from three germ layers [ Cell Death Discov, 2024, 10(1):95] | PubMed: 38388551 |
In Vitro Modelling of Osteogenesis Imperfecta with Patient-Derived Induced Mesenchymal Stem Cells [ Int J Mol Sci, 2024, 25(6)3417] | PubMed: 38542391 |
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432] | PubMed: 38464226 |
Transplantation of neural stem progenitor cells from different sources for severe spinal cord injury repair in rat [ Bioact Mater, 2023, 23:300-313] | PubMed: 36439085 |
Immuno-metabolic dendritic cell vaccine signatures associate with overall survival in vaccinated melanoma patients [ Nat Commun, 2023, 10.1038/s41467-023-42881-4] | PubMed: 37938561 |
Pathogenesis-related protein 1 suppresses oomycete pathogen by targeting against AMPK kinase complex [ J Adv Res, 2023, 43:13-26] | PubMed: 36585103 |
Cold exposure protects against medial arterial calcification development via autophagy [ J Nanobiotechnology, 2023, 21(1):226] | PubMed: 37461031 |
Interleukin-37 promotes DMBA/TPA skin cancer through SIGIRR-mediated inhibition of glycolysis in CD103+DC cells [ MedComm (2020), 2023, 4(2):e229] | PubMed: 36891351 |
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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