NPT1220-312, a TLR2/TLR9 Small Molecule Antagonist, Inhibits Pro-Inflammatory Signaling, Cytokine Release, and NLRP3 Inflammasome Activation

Figure 1

NPT1220-312 selectively inhibits TLR2 and TLR9. NPT1220-312 inhibition of (a) TLR1/2 as activated by Pam₃CSK₄ and TLR2/6 as activated by Pam₂CSK₄ in HEK293 cells overexpressing hTLR2; (b) TLR3 as activated by Poly I:C in HEK293 cells overexpressing hTLR3; (c) TLR4 as activated by LPS in HEK293 cells overexpressing hTLR4; (d) TLR7 as activated by R848 and as activated by CL-264 in HEK293 cells overexpressing hTLR7; (e) TLR8 as activated by R848 in HEK293 cells overexpressing hTLR8; and (f) TLR9 as activated by ODN2006 in HEK293 cells overexpressing hTLR9. TNFα was incorporated as a control for non-specific inhibition of signaling in each assay.

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