ML-T7 是一种有效的 Tim-3 抑制剂,阻断 Tim-3 与 PtdSer 和 CEACAM1 的相互作用,增强 CTLs 和 CAR T 细胞过继转移治疗的抗肿瘤活性及 T 细胞的效应功能,促进 NK 细胞对肿瘤细胞的杀伤活性和 DC 抗原呈递能力;单独使用或与 Nivolumab 联合使用可在临床前肿瘤模型中发挥抗肿瘤功效。ML-T7 可用于肿瘤免疫治疗研究。
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.
ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.