SML3121

TETi76 diethyl ester

Name: TETi76 diethyl ester
Brand: SIGMA

≥95% (HPLC)

别名:

2-Hydroxy-4-methylene-pentanedioic acid, 1,5-diethyl ester, AD145, Diethyl 2-hydroxy-4-methylenepentanedioate, TETi76 ester

登录查看组织和合同定价。

选择尺寸

关于此项目

经验公式（希尔记法）:

C₁₀H₁₆O₅

化学文摘社编号:

1451750-73-4

分子量:

216.23

NACRES:

NA.77

UNSPSC Code:

12352108

主要文件

查看所有文档

技术服务

需要帮助？我们经验丰富的科学家团队随时乐意为您服务。

让我们为您提供帮助

技术服务

需要帮助？我们经验丰富的科学家团队随时乐意为您服务。

让我们为您提供帮助

assay

≥95% (HPLC)

form

oil

color

colorless to yellow

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell-permeant, α-KG-competitive and hightly selective TET1/2/3 inhibitor with preferential cytotoxicity against TET-deficient cells in vitro and in vivo.

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.).