受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H14N2Na2O9S2 |
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分子量 | 548.45 | CAS No. | 20324-87-2 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL warmed with 50ºC water bath (182.33 mM) | |
Water | 22 mg/mL (40.11 mM) | |||
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 | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. |
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in vitro | In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. AMI-1 also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. [1] In addition, AMI-1 inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. [2] In INS-1 cells, AMI-1 improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation. [4] |
in vivo | In chronic AIPI rats, AMI-1 (5 μg/rat) ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs. [3] |
キナーゼアッセイ | In Vitro Methylation Assay | |
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All methylation reactions are carried out in the presence of S-adenosyl-L-[methyl-3H]methionine ([3H]AdoMet, 79 Ci/mmol from a 12.6 μM stock solution in dilute HCl/ethanol 9:1, pH 2.0–2.5) and PBS (137 mM NaCl, 2.7 mM KCl, 4.3 mM Na2HPO4, 1.4 mM KH2PO4, pH 7.4). The reactions are performed in a 30-μL volume in the presence of 5 μg of the small molecule inhibitors, this translates into the following concentration of each compound: AMI-1, 303 μM; AMI-2, 642 μM; AMI-3, 690 μM; AMI-4, 520 μM; AMI-5, 257 μM; AMI-6, 336 μM; AMI-7, 265 μM; AMI-8, 247 μM; AMI-9, 325 μM; AMA-1, 439 μM; AMA-2, 503 μM; and sinefungin, 437 μM. Additional information pertaining to individual reaction conditions is described in each of the figure legends. The samples are separated on a 10% SDS-PAGE, transferred to a PVDF membrane, sprayed with Enhance™, and exposed to film overnight. Band intensities are calculated using a Kodak Image Station 440 and 1D Image Analysis Software. | ||
動物実験 | 動物モデル | Chronic AIPI rats |
投薬量 | 50 μL at a concentration of 0.1 mg/mL | |
投与方法 | Intranasal injection |
Data from [Data independently produced by , , Nitric Oxide, 2017, 1-10]
PRMT1 reverts the immune escape of necroptotic colon cancer through RIP3 methylation [ Cell Death Dis, 2023, 14(4):233] | PubMed: 37005412 |
Methylation of HBP1 by PRMT1 promotes tumor progression by regulating actin cytoskeleton remodeling [ Oncogenesis, 2022, 11(1):45] | PubMed: 35941115 |
PRMT1 enhances oncogenic arginine methylation of NONO in colorectal cancer [ Oncogene, 2021, 40(7):1375-1389] | PubMed: 33420374 |
PRMT1 enhances oncogenic arginine methylation of NONO in colorectal cancer [ Oncogene, 2021, 10.1038/s41388-020-01617-0] | PubMed: 33420374 |
Hypoxia stimulates SUMOylation-dependent stabilization of KDM5B [ Research Square, 2021, 10.21203/rs.3.rs-620216/v1] | PubMed: None |
CARM1 Methylates GAPDH to Regulate Glucose Metabolism and Is Suppressed in Liver Cancer. [ Cell Rep, 2018, 24(12):3207-3223] | PubMed: 30232003 |
The asymmetric dimethylarginine-mediated inhibition of nitric oxide in the rostral ventrolateral medulla contributes to regulation of blood pressure in hypertensive rats. [Tan X, et al. Nitric Oxide, 2017, 67:58-67] | PubMed: 28392446 |
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。