CU-T12-9 是一种特异性TLR1/2激动剂，EC50为 52.9 nM。CU-T12-9 既激活先天免疫系统，又激活适应性免疫系统。CU-T12-9 选择性激活 TLR1/2 异二聚体而对 TLR2/6 没有作用。CU-T12-9 通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号，致使下游 TNF-α，IL-10，和 iNOS 增加，从而提高身体的免疫反应。
| 生物活性 | CU-T12-9 is a specificTLR1/2agonist withEC50of 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 throughNF-κBand invokes an elevation of the downstream effectors TNF-α,IL-10, andiNOS[1]. |
| IC50& Target[1] | TLR2 52.9 nM (EC50, in HEK-Blue cells) | TLR1 52.9 nM (EC50, in HEK-Blue cells) |
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体外研究
(In Vitro) | 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[1].
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[1].
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[1].
Cell Cytotoxicity Assay[1] | 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[1] | Cell Line: | Raw 264.7 cells | | Concentration: | 0.1, 1, 10 μM | | Incubation Time: | 24 hours for TLR1 and iNOS mRNA assay
2 hours for TLR2 and IL-10 mRNA assay
8 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(690.02 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7601 mL | 13.8003 mL | 27.6007 mL | | 5 mM | 0.5520 mL | 2.7601 mL | 5.5201 mL | | 10 mM | 0.2760 mL | 1.3800 mL | 2.7601 mL |
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