5.30154

BMI-1 Expression Inhibitor, PTC-209

• 别名: BMI-1 Expression Inhibitor, PTC-209, FLVI2/BMI1 Expression Inhibitor, MGC12685 Expression Inhibitor, PCGF4 Expression Inhibitor, PTC209; RNF51 Expression Inhibitor
• 经验公式（希尔记法）: C₁₇H₁₃Br₂N₅OS
• CAS号: 315704-66-6
• 分子量: 495.19
• MDL號碼: MFCD02110649
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥95% (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: light yellow
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C
• InChI: 1S/C17H13Br2N5OS/c1-9-15(24-5-3-4-20-16(24)21-9)13-8-26-17(22-13)23-14-11(18)6-10(25-2)7-12(14)19/h3-8H,1-2H3,(H,22,23)
• InChI 密鑰: XVOOCQSWCCRVDY-UHFFFAOYSA-N

说明

一般說明

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.

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).

生化／生理作用

Cell permeable: yes

Reversible: no

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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

法律資訊

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

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