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SR9243

SR9243

产品编号 T1801   CAS 1613028-81-1

SR9243 是一种 liver-X-receptor 的反向激动剂,可诱导 LXR-辅阻遏物相互作用。

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SR9243 Chemical Structure
SR9243, CAS 1613028-81-1
规格 价格/CNY 货期 数量
2 mg ¥ 275 现货
5 mg ¥ 452 现货
10 mg ¥ 651 现货
25 mg ¥ 1,190 现货
50 mg ¥ 1,970 现货
100 mg ¥ 3,390 现货
200 mg ¥ 4,920 现货
1 mL * 10 mM (in DMSO) ¥ 623 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: SR9243 (T1801)
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纯度: 99.03%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.
体外活性 In HEK293 cells expressing LXRs, SR9243 inhibits LXR activation by enhancing LXR-corepressor recruitment. In a variety of cancer cell types, SR9243 reduces cancer cell viability, induces apoptotic cell death, and sensitizes cancer cells to chemotherapeutic treatments. [1]
体内活性 In Ob/Ob mice fed a high-fat diet, SR9243 (60 mg/kg, i.p.) inhibits LXR-dependent lipogenic enzyme gene expression and tumor growth. [1]
激酶实验 ALK5 Fluorescence Polarization Binding Assay: GW788388 binding to ALK5 is tested on purified recombinant GST?ALK5 (residues 198-503). Displacement of rhodamine green fluorescently labeled ATP competitive inhibitor by different concentrations of GW788388 is used to calculate a binding pIC50. GST?ALK5 is added to a buffer containing 62.5 mM N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid (Hepes), pH 7.5, 1 mM dithiothreitol (DTT), 12.5 mM MgCl2, 1.25 mM 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonic acid (CHAPS), and 1 nM rhodamine green-labeled ligand so that the final ALK5 concentration is 10 nM based on active-site titration of the enzyme. The enzyme/ligand reagent (40 μL) is added to 384-well assay plates containing 1 μL of different concentrations of GW788388. The plates are read immediately on a LJL Acquest fluorescence reader with excitation, emission, and dichroic filters of 485, 530, and 505 nm, respectively. The fluorescence polarization for each well is calculated by the Acquest and is then imported into curve-fitting software for construction of concentration?response curves.
细胞实验 Cells are cultured in 96 well plates and treated with designated amounts of SR9243 for 96 hr in media containing 1% FBS and antibiotics. Cell-viability is assessed using the Cell-titre 96 kit according to the manufacturer's guidelines. Cell culture media is supplemented with oleate, stearate and palmitate dissolved in methanol to a concentration of 25 mM. 25 mM stocks are then diluted 10 fold in PBS containing 0.9% BSA. Lipid stocks (100X) are stored at ?20° until needed.(Only for Reference)
分子量 626.62
分子式 C31H32BrNO4S2
CAS No. 1613028-81-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 12.5 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5959 mL 7.9793 mL 15.9586 mL 39.8966 mL
5 mM 0.3192 mL 1.5959 mL 3.1917 mL 7.9793 mL
10 mM 0.1596 mL 0.7979 mL 1.5959 mL 3.9897 mL
20 mM 0.0798 mL 0.399 mL 0.7979 mL 1.9948 mL

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TargetMol Library Books参考文献

1. Flaveny CA, et al. Cancer Cell. 2015, 28(1), 42-56 2. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease[J]. Bioorganic chemistry. 2019 Mar;84:87-97.

TargetMol Library Books文献引用

1. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease. Bioorganic Chemistry. 2019 Mar;84:87-97
Gymnestrogenin XL041 AZ876 Gymnemagenin Ethyl 2,4,6-trihydroxybenzoate BMS-779788 Licochalcone E LXR-623

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌化合物库 代谢化合物库 已知活性化合物库 经典已知活性库 NO PAINS 化合物库 脂代谢化合物库 核受体化合物库 活性脂质化合物库 抗代谢疾病化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

SR9243 1613028-81-1 Metabolism Liver X Receptor SR-9243 LXR Liver X receptor Inhibitor SR 9243 inhibit inhibitor

 

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