TIM-3-IN-2 (Compound A-41) is a Tim3 inhibitor (KD: 0.61 μM). TIM-3-IN-2 blocks TIM-3 interactions with PtdSer, CEACAM1, and Gal-9. TIM-3-IN-2 inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 reverses the TIM-3-mediated blockade of the production of proinflammatory cytokines, and maximizes the T-cell antitumor activity against AML cell lines.
References:
[1]. Abdel-Rahman SA, et al. Discovery of Small-Molecule TIM-3 Inhibitors for Acute Myeloid Leukemia Using Pharmacophore-Based Virtual Screening. J Med Chem. 2023 Aug 24;66(16):11464-11475.