TIM-3 inhibitor A-41 is small-molecule inhibitor of T-cell immunoglobulin and mucin domain 3 (TIM-3; HAVCR2) with SPR Kd value of 0.61 uM.
TIM-3 inhibitor A-41 displays minimal inhibitory profile against a panel of immune checkpoints, including PD-1, CTLA4, LAG-3, VISTA, and TIGIT.
TIM-3 inhibitor A-41 demonstrates a remarkable ability to block TIM-3/CEACAM1 and TIM-3/PtdSer interactions at submicromolar concentrations, blocks the TIM-3/Gal-9 interaction in a cellular platform at 1 μM.
TIM-3 inhibitor A-41 decreases the proliferation of THP-1 cells in a similar pattern to anti-TIM-3 mAb.
TIM-3 inhibitor A-41 rescues IFNγ (interferon γ) release from peripheral blood mononuclear cells (PBMCs) inhibited by recombinant TIM-3.
TIM-3 inhibitor A-41 (5 uM) potentiates the ability of PBMCs to significantly inhibit the proliferation of Kasumi-1 cells (AML cell line) in the PBMCs/Kasumi-1 coculture assay.