ask1-in-1

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.

ASK1-IN-10 (Compound 27) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of less than 200 nM. It also exhibits inhibitory activity on the hERG potassium channel. ASK1-IN-10 is utilized in inflammation research.

ASK1-IN-11 (Compound 7) is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of less than 200 nM. It also exhibits inhibitory activity against TNF-α, MYLK/MLCK kinase, and the hERG potassium ion channel. ASK1-IN-11 can be utilized in inflammation research.

ASK1-IN-12 is an ASK1 inhibitor with an IC50 of 6.3 nM. It effectively suppresses the activation of the ASK1-p38/JNK pathway induced by TNF-α. Additionally, ASK1-IN-12 reduces cholesterol elevation and lipid droplet accumulation induced by free fatty acids, improving hepatic steatosis. This compound is valuable for research on non-alcoholic steatohepatitis (NASH).

TASK-1-IN-1 is a potent and selective inhibitor of TASK-1 (Potassium Channel) with an IC50 of 148 nM, and exhibits a reduced inhibitory effect on the TASK-3 channel with an IC50 of 1750 nM. TASK-1-IN-1 also demonstrates anticancer effects.

ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.

ASK1-IN-9 (Compound 3) is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of less than 200 nM. It is applicable for inflammation research.

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), a selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor, exhibits an IC50 of 25 nM. This compound readily crosses the blood-brain barrier, as evidenced by rat pharmacokinetics showing a clearance/unchanged clearance rate of 1.6/56 L/h/kg and an unbound partition coefficient (Kp,uu) of 0.46. Additionally, ASK1-IN-6 demonstrates anti-inflammatory activity and effectively improves symptoms in the Alzheimer's Disease Tg4510 mouse model.

ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1].