260921

DNA Methyltransferase Inhibitor II, SGI-1027

• 同義詞: DNA Methyltransferase Inhibitor II, SGI-1027, N-(4-(2-Amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)-benzamide, S-1027, DNA MTase Inhibitor II
• 經驗公式（希爾表示法）: C₂₇H₂₃N₇O
• 分子量：: 461.52
• 分類程式碼代碼: 12352200

屬性

• 化驗: ≥88% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: pale yellow
• 溶解度: DMSO: 50 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C

描述

一般說明

A cell-permeable quinoline compound that is shown to inhibit human DNMT1 (IC₅₀ = 6 and 12.5 µM, respectively, with Hemimethylated DNA or Poly(dI-dC) as the substrate), murine DNMT3a & 3b (IC₅₀ = 8 and 7.5 µM, respectively, with Poly(dI-dC) as the substrate), as well as CpG DNA methylase M.SssI (IC₅₀ = 13.5 and 16 µM, respectively, with Poly(dI-dC) as the substrate and 75 or 150 nM AdoMet) of mycoplasma Spiroplasma sp. strain MQ1, presumably by competing with AdoMet (S-adenosyl-L-methionine , SAM) for the enzyme′s cofactor binding site. Shown to be 2-, 3-, and 5-fold more effective than Decitabine (Cat. No. 189825), respectively, in reactivating p16 mRNA (2.5 µM for 7 days), MLH1 mRNA (2.5 µM for 7 days), and p16 protein expression (1.0 or 2.5 µM for 12 days) in human colon carcinoma RKO cultures by reducing CpG island hypermethylation found in the promoter regions of TSGs (tumor suppressor genes) without inducing genome-wide hypomethylation or caspase-3 activation.

A cell-permeable quinoline compound that is shown to inhibit human DNMT1 (IC₅₀ = 6 and 12.5 µM, respectively, with Hemimethylated DNA or Poly(dI-dC) as the substrate), murine DNMT3a & 3b (IC₅₀ = 8 and 7.5 µM, respectively, with Poly(dI-dC) as the substrate), as well as CpG DNA methylase M.SssI (IC₅₀ = 13.5 and 16 µM, respectively, with Poly(dI-dC) as the substrate and 75 or 150 nM AdoMet) of mycoplasma Spiroplasma sp. strain MQ1, presumably by competing with AdoMet (S-adenosyl-L-methionine , SAM) for the enzyme′s cofactor binding site. Shown to be 2-, 3-, and 5-fold more effective than Decitabine (Cat. No. 189825), respectively, in reactivating p16 mRNA (2.5 µM for 7 days), MLH1 mRNA (2.5 µM for 7 days), and p16 protein expression (1.0 or 2.5 µM for 12 days) in human colon carcinoma RKO cultures by reducing CpG island hypermethylation found in the promoter regions of TSGs (tumor suppressor genes) without inducing genome-wide hypomethylation or caspase-3 activation.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

Datta, J., et al. 2009. Cancer Res.69, 4277.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable