ask1-in-1

ASK1-IN-1 是一种凋亡信号调节激酶 1（SK1） 抑制剂，具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。

TASK-1-IN-1 是一种有效的选择性的 TASK-1 (Potassium Channel) 抑制剂（IC50 ： 148 nM）。TASK-1-IN-1 对 TASK-3 通道 的IC50 为 1750 nM，抑制作用有所降低。TASK-1-IN-1 具有抗癌作用。

ASK1-IN-3 is a highly potent and selective inhibitor of ASK1 kinase, demonstrating an IC 50 of 33.8 nM. This compound also exhibits inhibitory effects on various cell cycle regulating kinases. ASK1-IN-3 showcases remarkable induction of apoptosis in HepG2 cancer cells and displays potent activity in arresting the cell cycle [1].

BPyO-34 is a novel apoptosis signal-regulating kinase 1 (ASK1) inhibitor with IC50 of 0.52μM in vitro in kinase assay.

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

ASK1-IN-6 (Compound 32) 是一种针对凋亡信号调节激酶 1 (ASK1) 的选择性抑制剂，具有 25 nM 的半抑制浓度 (IC50)。此化合物表现出良好的血脑屏障渗透性（大鼠动脉 静脉清除率为 1.6 56 L h kg，脑间隙非离子型药物分配系数 (Kp,uu) 为 0.46）。在阿尔茨海默症的 Tg4510 小鼠模型中，ASK1-IN-6 显示了其抗炎效果并有助于疾病的改善。

ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。