| 产品描述： | CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS |
| 靶点： |
TLR2:52.9 nM (EC50, in HEK-Blue cells);TLR1:52.9 nM (EC50, in HEK-Blue cells) |
| 体外研究： |
CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling. CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α[1].CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells. CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours. Cell Cytotoxicity Assay Cell Line: HEK-Blue hTLR2 and Raw 264.7 macrophage cells Concentration: 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50, and 100 μM Incubation Time: 24 hours Result: No toxicity was seen up to 100 μM. RT-PCR Cell Line: Raw 264.7 cells Concentration: 0.1, 1, 10 μM Incubation Time: 24 hours for TLR1 and iNOS mRNA assay2 hours for TLR2 and IL-10 mRNA assay8 hours for TNF mRNA assay Result: Triggered TLR1 mRNA and iNOS mRNA at 24 hours dose-dependently.Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hours.Showed dose-dependent activation of TNF mRNA at 8 hours. |
| 参考文献： |
1. Cheng K, Gao M, Godfroy JI, Brown PN, Kastelowitz N, Yin H. Specific activation of the TLR1-TLR2 heterodimer by small-molecule agonists. Sci Adv. 2015;1(3). pii: e1400139. PubMed PMID: 26101787; PubMed Central PMCID: PMC4474499. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.76 ml |
13.8 ml |
27.601 ml |
| 5 mM |
0.552 ml |
2.76 ml |
5.52 ml |
| 10 mM |
0.276 ml |
1.38 ml |
2.76 ml |
| 50 mM |
0.055 ml |
0.276 ml |
0.552 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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