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Potency of small molecule TLR agonists in activating TLR7- and TLR8-mediated NF-κB activity in transfected human HEK293 cells. |
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| Compound |
Minimum effective concentration (MEC, μM) for NFκB activation (a) |
TLR selectivity (b) |
|
|
|
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| TLR7 |
TLR8 |
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|
|
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| 3M-006 |
Inactive (100) |
Inactive (100) |
None |
| 3M-003 |
0.1 |
1 |
TLR7/8 @ 1 μM |
| 852A |
3 |
100 |
TLR7 @ 3 μM |
| 3M-002 |
10 |
1 |
TLR8 @ 5 μM |
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(a) Transfection of HEK293 cells with TLR7 or TLR8, and assessment of IRM-induced NFκB activation was performed as previously described [6]. Potency is defined as the concentration required to induce an increase in NFκB activation. MEC, minimal effective concentration, is the lowest concentration required to observe a 2-fold increase above the vehicle control. (b) Selectivity is defined as preferential signaling through TLR7 or TLR8 at a specified concentration of the TLR agonists. | |||
Hanten et al. BMC Immunology 2008 9:39 doi:10.1186/1471-2172-9-39 |
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