AMI-1

製品コードS7884 バッチS788401

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

C21H14N2Na2O9S2
分子量 548.45 CAS No. 20324-87-2
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 100 mg/mL (182.33 mM)
Water 22 mg/mL (40.11 mM)
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 AMI-1は、酵母Hmt1pおよびヒトPRMT1に対し、それぞれ3.0 µMおよび8.8 µMのIC50を示す、強力かつ特異的なヒストンメチルトランスフェラーゼ（HMT）阻害剤です。
in vitro In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. This compound also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. In addition, it inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. In INS-1 cells, this chemical improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation.
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.

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Methylation Assay
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; this compound, 642 μM; this compound, 690 μM; this compound, 520 μM; this compound, 257 μM; this compound, 336 μM; this compound, 265 μM; this compound, 247 μM; this compound, 325 μM; this compound, 439 μM; this compound, 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

参考

  • https://pubmed.ncbi.nlm.nih.gov/15056663/
  • https://pubmed.ncbi.nlm.nih.gov/12642128/
  • https://pubmed.ncbi.nlm.nih.gov/26026059/
  • https://pubmed.ncbi.nlm.nih.gov/25874535/

カスタマーフィードバック

Data from [Data independently produced by , , Nitric Oxide, 2017, 1-10]

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：

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 [ Front Cell Dev Biol, 2021, 9:741736] PubMed: 34977006
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。

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