产品说明

一般描述

A cell-permeable imidazopyrimidinyl-thiazolamine compound that effectively downregulates cellular BMI-1 protein level both in cultures in vitro (IC₅₀ = 0.5 µM/48 h/HT1080 and <0.37 µM/HCT116/overnight) and in mice in vivo (60 mg/kg/d via s.c.) by inhibiting BMI-1 transcription via a yet unidentified mechanism, thereby reducing BMI-1-dependent RING1A E3 ligase activity and RING1A-mediated H2A ubiquitination (uH2A)/epigenetic regulations. Shown to exhibit antiproliferation activity against human colon cancer cells both in cultures (IC₅₀<300 nM) in vitro and in mice (30 to 60 mg/kg/d s.c.) in vivo via G0 cell cycle arrest and apoptosis induction with a greater drug impact on self-renewing cancer-initiating cells (CICs; cancer stem cells).
A cell-permeable imidazopyrimidinyl-thiazolamine compound that effectively downregulates cellular BMI-1 protein level both in cultures in vitro (IC₅₀ = 0.5 µM/48 h/HT1080 and <0.37 µM/HCT116/overnight) and in mice in vivo (4.5 ng vs.13.7 ng per mg HT1080 tumor tissue, respectively, with or without 10-d 60 mg/kg/d treatment via s.c.) by inhibiting BMI-1 transcription (IC₅₀ = 0.5 µM against overnight reporter transcription in HEK293) via a yet unidentified mechanism, thereby reducing BMI-1-dependent RING1A E3 ligase activity and RING1A-mediated H2A ubiquitination (uH2A)/epigenetic regulations. Shown to exhibit antiproliferation activity against human colon cancer cells both in cultures (IC₅₀<300 nM against LS174T and primary colon cancer cultures) in vitro and in mice (30 to 60 mg/kg/d s.c.) in vivo by inducing cell cycle arrest at G₀ and apoptosis. Reduced frequency of sphere-forming cells is observed among surviving cells (by 1.7- to 2.2-fold) upon PTC-209 removal post a 4-day 0.1 µM drug treatment period in primary colon cancer cultures, indicating a greater impact of drug treatment on self-renewing cancer-initiating cells (CICs; cancer stem cells). Likewise, surviving colon cancer cells from tumor-bearing mice at the end of drug treatment are shown to contain reduced population of tumor-initiating cells when xenografted into secondary recipient mice.

生化/生理作用

Cell permeable: yes
Reversible: no

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Kreso, A., et al. 2014. Nat. Med.20, 29.

法律信息

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

基本信息

产品性质

安全信息

产品说明

应用

PTC-209已被用作B淋巴瘤Mo-MLV插入区1同源物(BMI1)抑制剂，用于研究其对以下方面的影响：

• 犬骨肉瘤(OSA)细胞系的细胞活力
• 卵巢癌(OvCa)细胞中脂质化的微管相关蛋白1轻链3(LC3B-II)和死骨片1(SQSTM1)蛋白的水平
• 小鼠胚胎成纤维细胞(MEF)的心脏重编程效率

包装

5, 25 mg in glass bottle

生化/生理作用

PTC-209 抑制癌基因 BMI-1(B 淋巴瘤 Mo-MLV 插入区 1 同源物)的表达，该基因编码参与细胞周期的多梳环 RING 指蛋白。 PTC-209 降低结肠直肠癌起始细胞(CIC)的自我更新特性。该化合物抑制肿瘤生长，并降低小鼠结肠癌肿瘤异种移植物中 CIC 的水平。

特点和优势

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基本信息

产品性质

安全信息