tim-3-in-1

TIM-3-IN-1 is a useful tool to enable further studies on the biology of TIM-3 immunoregulation in cancer.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

ML-T7, a powerful inhibitor of Tim-3, effectively disrupts its interactions with PtdSer and CEACAM1. This compound enhances the antitumor activity of adoptive transfer therapy involving cytotoxic T lymphocytes (CTLs) and CAR T cells, while also boosting T cell effector functions. Additionally, ML-T7 augments the killing activity of NK cells against tumor cells and improves the antigen-presenting capacity of dendritic cells (DCs). Demonstrating antitumor efficacy in preclinical models, ML-T7 shows potential either as a standalone treatment or in combination with Nivolumab for tumor immunotherapy research [1].