tpca-1

TPCA-1 is a selective small molecule inhibitor of human IκB kinase 2 (IKKβ/IKK2), with an IC50 of approximately 17.9 nM. It inhibits the NF-κB signaling pathway by blocking the phosphorylation and degradation of IκBα, thereby preventing nuclear translocation of NF-κB and suppressing the transcription of pro-inflammatory cytokines such as TNFα, IL-6, and IL-8. TPCA-1 also reduces STAT3 activity by interfering with its recruitment to upstream kinases via interaction with the SH2 domain. This dual inhibition results in anti-inflammatory effects in animal models of arthritis and has shown potential for reducing inflammation in other conditions such as chronic periodontitis and post-traumatic osteoarthritis[1][2][6]. The drug is investigational and not approved for clinical use.

Other names

2-((aminocarbonyl)amino)-5-(4-fluorophenyl)-3-thiophenecarboxamide3-thiophenecarboxamide, 2-((aminocarbonyl)amino)-5-(4-fluorophenyl)-IKKβ inhibitor