NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-bindingoligomerization domain-like receptor 1/2) dual antagonist, with IC 50 values of 1.13 ( NOD1 ) and 0.77 μM ( NOD2 ), respectively. NOD1/2 antagonist-1 has a acceptable T 1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).