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CU-CPT17e Sale

目录号 : GC33834

CU-CPT17e是一种多Toll样受体(TLR)激动剂,可激活TLR3,TLR8和TLR9。

CU-CPT17e Chemical Structure

Cas No.:2109805-75-4

规格 价格 库存 购买数量
5mg
¥4,860.00
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10mg
¥7,200.00
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25mg
¥13,050.00
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50mg
¥21,310.00
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100mg
¥29,535.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Cell experiment:

HeLa cells are seeded at a density of 3×105 cells/well in 6-well plates and allowed to attach for 24 h. After treatment of indicated concentrations of CU-CPT17e or poly I:C (5 μg/mL) for another 24 h, cells are harvested with 0.25% trypsin without EDTA and rinsed twice with PBS, then stained using a Annexin V-FITC apoptosis detection kit. Cells are analyzed with a BD Accuri C6 flow cytometer[1].

References:

[1]. Zhang L, et al. Discovery of Small Molecules as Multi-Toll-like Receptor Agonists with Proinflammatory and Anticancer Activities. J Med Chem. 2017 Jun 22;60(12):5029-5044.

产品描述

CU-CPT17e is a multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.

CU-CPT17e shows strong NF-κB activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 μM, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-κB activation and an EC50 value of 4.8±0.7 μM. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 μM) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 μg/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1].

[1]. Zhang L, et al. Discovery of Small Molecules as Multi-Toll-like Receptor Agonists with Proinflammatory and Anticancer Activities. J Med Chem. 2017 Jun 22;60(12):5029-5044.

Chemical Properties

Cas No. 2109805-75-4 SDF
Canonical SMILES O=[N+]([O-])C(C=C1)=CC=C1COC2=CC(C=CC3(CCOCC3)O4)=C4C=C2OCC5=CC=C([N+]([O-])=O)C=C5
分子式 C27H24N2O8 分子量 504.49
溶解度 DMSO : 5 mg/mL (9.91 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9822 mL 9.911 mL 19.822 mL
5 mM 0.3964 mL 1.9822 mL 3.9644 mL
10 mM 0.1982 mL 0.9911 mL 1.9822 mL
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Research Update

Discovery of Small Molecules as Multi-Toll-like Receptor Agonists with Proinflammatory and Anticancer Activities

J Med Chem 2017 Jun 22;60(12):5029-5044.PMID:28537730DOI:10.1021/acs.jmedchem.7b00419

Therapies based on activation of multiple Toll-like receptors (TLRs) may offer superior therapeutic profiles than that of single TLR activation. To discover new small molecules that could activate multiple TLRs, we performed a cell-based high-throughput screening of a small-molecule library based on TLR3-mediated NF-κB activation. Subsequent structural optimization and counterscreening of other TLRs produced the first small molecule 17e (CU-CPT17e) capable of simultaneously activating TLRs 3, 8, and 9. Biochemical studies demonstrated that 17e could induce a strong immune response via the production of various cytokines in human monocytic THP-1 cells. Furthermore, 17e inhibited the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. These results showcase potential therapeutic applications of 17e in both vaccine adjuvants and anticancer therapies based on multi-TLR activation.