1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. CU-T12-9

CU-T12-9 

Cat. No.: HY-110353
Handling Instructions

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.

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CU-T12-9 Chemical Structure

CU-T12-9 Chemical Structure

CAS No. : 1821387-73-8

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Description

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[1].

IC50 & Target[1]

TLR2

52.9 nM (EC50, in HEK-Blue cells)

TLR1

52.9 nM (EC50, in HEK-Blue cells)

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.
Molecular Weight

362.31

Formula

C₁₇H₁₃F₃N₄O₂

CAS No.

1821387-73-8

SMILES

CNC1=CC=C(C=C1N2C=C(N=C2)C3=CC=C(C=C3)C(F)(F)F)[N+]([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

CU-T12-9Toll-like Receptor (TLR)specificTLR1/2 inflammatoryinfectiousdiseasesinfluenzaasthmaobesitybreastcancerbladderpancreaticcarcinomaInhibitorinhibitorinhibit

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