ASK1

ASK1-IN-4 是一种ASK1抑制剂，IC50 = 0.2 μM。

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。

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。

NQDI-1 (NQDI 1) 是一种凋亡信号调节激酶 1 抑制剂，Ki 为 500 nM，IC50为 3 μM。

TC ASK 10 是选择性的，口服有效的细胞凋亡信号调节激酶 1 抑制剂，IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50％，除 ASK2之外 (IC50为 0.51 μM)。

MSC 2032964A 是一种有效的选择性 ASK1 抑制剂 (IC50 = 93 nM)，具有口服生物利用度和脑渗透性。它在小鼠 EAE 模型中抑制神经炎症，并在培养的小鼠星形胶质细胞中阻断 LPS 诱导的 ASK1 和 p38 磷酸化。

GS-444217 是一种可口服的选择性 ATP 竞争性凋亡信号调节激酶 1 抑制剂，IC50为 2.87 nM。

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-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].

ASK1-IN-7 (Compound 4c) 是一种ASK1抑制剂，源于ASK1抑制剂支架 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one 衍生物。ASK1-IN-7 适用于研究与ASK1信号通路相关的领域，包括细胞应激反应、炎症反应、神经退行性疾病以及心血管疾病等。

Selonsertib (GS-4997) 是一种选择性的，具有生物口服可利用的凋亡信号调节激酶1 抑制剂，pIC50为 8.3。它具有潜在的抗炎、抗肿瘤和抗纤维化活性。

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。

JT21-25 (compound 9h) 作为一种高效的选择性凋亡信号调节激酶 1 (ASK1) 抑制剂，其 IC50 值为 5.1 nM。

A1899 is a effective and selective TASK-1 and TASK-3 antagonist.

Doxapram hydrochloride hydrate (Doxapram HCl) 是 TASK-1，TASK-3和 TASK-1 TASK-3异二聚体通道的抑制剂，EC50分别为410 nM，37 μM 和9 μM。

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) 作为一种有效的蛋白激酶抑制剂，展现了对PKC-α、ROCK、ASK1的强效抑制作用，其IC50分别为0.092, 0.26, 0.77 μM。此外，该化合物对PC-3癌细胞线具有显著的细胞毒性，其IC50为0.16 μM。

(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde (MDA) and decreases in superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities as well as increases constitutive nitric oxide synthase (cNOS) activity and nitric oxide (NO) production in HUVECs. CSTMP also induces cell death of A549 non-small cell lung cancer (NSCLC) cells in an IRE1α-dependent manner through induction of IRE1α-TRAF2-ASK1 complex-mediated endoplasmic reticulum (ER) stress and mitochondrial apoptosis.

Antagonist of 14.3.3 proteins (KD ≈80 nM). Competitively inhibits 14.3.3-ligand interactions without requiring phosphorylation. Blocks the ability of 14.3.3 to bind to target proteins such as Raf-1, Bad, ASK1 and exoenzyme S.

K812 is an ASK1-specific inhibitor discovered to prolong survival in a mouse model of amyotrophic lateral sclerosis.

Sulfotanshinone IIA Sodium mitigates oxidative damage in peritoneal mesothelial cells caused by peritoneal dialysis solution (PDS) by inhibiting the ASK1-p38 signaling pathway.

CS17919 (0.32-10 µM；72小时) 对经棕榈酸处理的LO2细胞展现出显著的保护效果。

DDO3711是通过化学接头将ASK1 (小分子凋亡信号调节激酶1) 抑制剂与PP5 (磷酸酶) 激活剂连接，形成特定于招募PP5的磷酸酶募集嵌合体(PHORC)。该化合物特异性地抑制ASK1 (IC50=164.1 nM)，而对ASK2 (IC50>20 μM)无影响。通过募集PP5，DDO3711显著促进p-ASK1T838的去磷酸化，表现出ASK1依赖性的抗增殖活性，显示其抗癌潜力并可用于研究异常磷酸化癌蛋白。

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.

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