ido/tdo-in-1

IDO TDO-IN-1 is an orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50s: 9.7 and 47 nM).

(R)-IDO/TDO-IN-1 (化合物 25) 为一种具有优良药动学性质的吲哚胺-2,3-双加氧酶 (IDO) 抑制剂，在MC38异种移植模型中展现出抗肿瘤活性。该化合物还与抗PD-1单克隆抗体 (SHR-1210) 显示协同作用。

IDO1 TDO-IN-1 (30) is a highly effective inhibitor that targets both IDO1 and TDO enzymes with uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound, IDO1 TDO-IN-1 (30), exhibits a significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2 Bax pathway [1].

IDO Tubulin-IN-2 (HT2) 是一种对TDO和微管蛋白 (tubulin)展现出高效抑制作用的化合物。该抑制剂对多种癌细胞系（包括U87、HepG2、A549、HCT-116和LO2）均表现出强抗肿瘤活性，其半抑制浓度（IC50）分别为0.43、0.036、0.041、0.095和1.04 μM，有效提升了抗肿瘤效果。