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BMI-1 Expression Inhibitor, PTC-209，10MG，5301540001，Sigma

销售价： ¥ 2226.48 / 件

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订货号： 0BP8339

品牌型号： Sigma 5301540001

货期：询货期

最小订货量： 1件

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商品介绍
规格参数
包装参数

产品介绍 Product Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Reversible: no

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

技术参数 Specifications

assay	≥95% (HPLC)
Quality Segment	100
form	powder
manufacturer/tradename	Calbiochem^®
storage condition	OK to freeze,protect from light
color	light yellow
solubility	DMSO: 100 mg/mL
storage temp.	2-8°C
SMILES string	[s]1c(nc(c1)c3[n]4c(nc3C)nccc4)Nc2c(cc(cc2Br)OC)Br
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 key	XVOOCQSWCCRVDY-UHFFFAOYSA-N

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