iST2-1

iST2-1 is an Stimulation-2 (ST2) inhibitor with an IC₅₀ value of 46.65 μM, blocks interaction between ST2 and IL-33, inhibits downstream signaling. iST2-1 functions as an immunomodulator, reduces proliferation of CD4⁺ and CD8⁺ T cells, increases regulatory T cell populations, reduces IFN-γ⁺CD4⁺ T cell populations, increases Foxp3⁺CD4⁺ regulatory T cell populations in the gastrointestinal tract. iST2-1 reduces plasma soluble ST2 and IFN-γ levels, reduces graft-versus-host disease scores, improves survival in graft-versus-host disease animal models, preserves graft-versus-tumor effect. iST2-1 can be used for the research of graft-versus-host disease^[1][2]. In Vitro:iST2-1 inhibits ST2/IL-33 binding in the AlphaLISA assay with an IC₅₀ of 46.65 μM^[1].
iST2-1 inhibits ST2/IL-33 signaling in HEK-Blue^TM IL-33 cells with an IC₅₀ range of 56.42-65.87 μM^[1].
iST2-1 (1 μM) exhibits short metabolic stability in both mouse and human liver microsomes with T_1/2 values of 0.73 min and 1.10 min, respectively^[1]. In Vivo:iST2-1 (41.4 mg/kg; i.p.; daily; 21 days) reduces GVHD score to 3, maintains plasma hsST2 below 30 pg/mL through Day 28, and improves survival rate to 45% on Day 35 in NSG mouse GVHD models^[2].
iST2-1 reduces plasma sST2 concentration, decreases gastrointestinal IFNγ⁺CD4⁺ T cells, and increases gastrointestinal Foxp3⁺CD4⁺ Tregs in C3H.SW mouse GVHD models^[2].