SML3121

TETi76 diethyl ester

≥95% (HPLC)

• 别名: 2-Hydroxy-4-methylene-pentanedioic acid, 1,5-diethyl ester, AD145, Diethyl 2-hydroxy-4-methylenepentanedioate, TETi76 ester
• 经验公式（希尔记法）: C₁₀H₁₆O₅
• CAS号: 1451750-73-4
• 分子量: 216.23
• 分類程式碼代碼: 12352108
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: oil
• 顏色: colorless to yellow
• 儲存溫度: 2-8°C

说明

生化／生理作用

TETi76 diethyl ester is a cell-permeant diester form of the α-KG-competitive and hightly selective TET1/2/3 dioxygenase inhibitor TETi76 acid (TET2 cat. domain Kd = 0.3 μM; no potency against 16 other αKG/Fe2+-dependent enzymes, including closely related RNA dioxygenase FTO). TETi76 ester downregulates cellular 5-hydroxymethylcytosine (5hmC) levels (IC50 = 20-37 μM; K562, MEG01, SIGM5, OCI-AML5, MOLM13), exerts preferential cytotoxicity in TET-deficient cultures (TET2/3-knockout K562 LD50 ~10 μM vs wt K562 LD50 ~40 μM) and significantly reduces TET2-deficient SIGM5 tumor burden in mice in vivo (50 mg/kg p.o.).

安全信息

• 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