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].

iST2-1 在 AlphaLISA 实验中抑制 ST2/IL-33 的结合，其 IC₅₀ 为 46.65 μM^[1]。
iST2-1 可在 HEK-Blue^TM IL-33 细胞中抑制 ST2/IL-33 信号通路，其 IC₅₀ 范围为 56.42-65.87 μM^[1]。
iST2-1 (1 μM) 在小鼠和人肝微粒体中代谢稳定性较差，其 T_1/2 值分别为 0.73 min 和 1.10 min^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

iST2-1 (41.4 mg/kg；腹腔注射；每日给药；持续 21 天) 在 NSG 小鼠移植物抗宿主病 (GVHD) 模型中可将 GVHD 评分降至 3，在第 28 天时维持血浆 hsST2 水平低于 30 pg/mL，并在第 35 天时将存活率提升至 45%^[2]。
iST2-1 可降低 C3H.SW 小鼠移植物抗宿主病 (GVHD) 模型中的血浆 sST2 浓度，减少胃肠道 IFNγ⁺CD4⁺ T 细胞数量，并增加胃肠道 Foxp3⁺CD4⁺ Tregs 的数量^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

378.42

C₂₂H₂₂N₂O₄

1019158-02-1

液体（密度：1.235±0.06 g/cm³）

Room temperature in continental US; may vary elsewhere.

• [1]. Yuan X, et al. Structure-Activity relationship of 1-(Furan-2ylmethyl)Pyrrolidine-Based Stimulation-2 (ST2) inhibitors for treating graft versus host disease. Bioorg Med Chem. 2022;71:116942.

  [2]. Chao-Yie Yang, et al. Small Molecule ST2 Inhibitors Cause Reduction of Soluble ST2 and Improve Gvhd and Survival In Vivo.Blood Volume 128, Issue 22, 2 December 2016, Page 528.