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SR-9243
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR-9243图片
CAS NO:1613028-81-1
规格:98%
分子量:626.62
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
inverse agonist of LXR
CAS:1613028-81-1
分子式:C31H32BrNO4S2
分子量:626.62
纯度:98%
存储:Store at -20°C

Background:

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction. It potently reduces cancer cell viability (IC50=15–104 nM) in MTT reduction assays in prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. [1]


LXR (liver X receptor) is a member of the nuclear receptor family of transcription factors. It is an important regulator of glycolysis and lipogenesis enzyme expression.


In SW620 cells, 1 mM SR9243 treatment for 12 hours induces cell death with a robust increase in caspase 3/7 activation. In addition, SR9243 disrupts the Warburg effect, suppresses lipogenesis gene expression and lipid production in cancer cells without effecting normal cells. [1]


In colon tumor xenograft, SR9243 substantially and dose-dependently reduces tumor growth, glycolytic (GCK1, PFK2, PFK1 and LDH) and lipogenic (SCD1, FASN, and SREBP1c) enzyme expression without promoting weight loss. SR9243 also blocks tumor growth without causing immune or hepatic toxicity in vivo. [1]


Reference:
1.  Flaveny CA, Griffett K, El-Gendy Bel-D et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell. 2015 Jul 13;28(1):42-56.