ASK1 Inhibitor

Aceglutamide (α-N-Acetyl-L-glutamine; N2-Acetylglutamine) is a neuroprotectant that can penetrate the blood-brain barrier. Aceglutamide can enhance the antioxidant systems of glutathione (GSH), thioredoxin (Trx) and Nrf2. Aceglutamide also inhibits ASK1 and TRAF1, activates the Akt/Bcl-2 anti-apoptotic pathway, enhances the activity of antioxidant enzymes and reduces oxidative damage. Aceglutamide can improve neurological deficits after cerebral ischemia, reduce infarct volume, and inhibit neuronal apoptosis, especially substantia nigra dopaminergic neurons. Aceglutamide can reduce cerebral ischemia/reperfusion injury, improve motor dysfunction, and is used in ischemic stroke-related research.

ASK1-IN-6 is a selective, orally active, and blood-brain barrier penetrant inhibitor of ASK1 (biochemical IC₅₀: 7 nM; cellular IC₅₀: 25 nM). ASK1-IN-6 exhibits anti-inflammatory and can be used in the research of neurodegenerative diseases such as Alzheimer's disease.

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

GDC-3280 (AK3287; AKEX0011) is an orally active compound based on Pirfenidone (HY-B0673)'s phenyl pyridone scaffold. GDC-3280 alleviates the inflammatory and fibrotic reaction of silicosis by inhibiting the ASK1-p38 MAPK pathway and regulating macrophage polarization. GDC-3280 exhibits anti-inflammatory and anti-fibrotic effects.

BPyO-34 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 0.52 μM against human targets. BPyO-34 inhibits the activity of ASK1 in in vitro kinase assays. BPyO-34 can be used in research related to various diseases such as diabetes and cancer.

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC₅₀=138 nM; Biochemical IC₅₀=21 nM).

ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC₅₀=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1.

ASK1-IN-10 (Compound 27) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ <200 nM. ASK1-IN-10 also shows inhibitory activity to hERG potassium channels. ASK1-IN-10 can be used for the research of inflammation.

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 an experimental mouse model of liver injury induced by Acetaminophen (HY-66005), ASK1-IN-8 can significantly reduce the plasma alanine transaminase (ALT) level, protecting the liver. ASK1-IN-8 can be used in research related to liver diseases.

K811 is an orally active ASK1 inhibitor with an IC₅₀ of 6 nM. K811 inhibits glial cell activation in the lumbar spinal cord of SOD1^G93A transgenic mice. K811 extends the survival of SOD1^G93A transgenic mice, a mouse model of amyotrophic lateral sclerosis. K811 can be used in studies related to amyotrophic lateral sclerosis.

ASK1-IN-11 (Compound 7) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ <200 nM. ASK1-IN-11 also shows inhibitory activities to TNF-α, MYLK/MLCK Kinase and hERG potassium channels . ASK1-IN-11 can be used for the research of inflammation.

ASK1-IN-9 (Compound 3) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ <200 nM. ASK1-IN-9 can be used for the research of inflammation.

ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC₅₀ of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities.

ASK1-IN-12 is an ASK1 inhibitor with an IC₅₀ of 6.3 nM. ASK1-IN-12 inhibits TNF-α-induced activation of the ASK1-p38/JNK pathway. ASK1-IN-12 can reduce free fatty acid-induced cholesterol increase, lipid droplet accumulation and improves hepatocellular steatosis. ASK1-IN-12 can be used for the research of non-alcoholic steatohepatitis (NASH).

K812 is an orally active ASK1 inhibitor with a 6 nM IC₅₀ against ASK1. K812 selectively inhibits ASK1 activation. K812 inhibits glial activation in the lumbar spinal cord. K812 extends survival of SOD1^G93A transgenic mice. K812 can be used for the research of amyotrophic lateral sclerosis.

ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. ASK1-IN-7 holds promise for research related to the ASK1 signaling pathway, such as cell stress responses, inflammation, neurodegenerative diseases, and cardiovascular diseases.

ASK1-IN-5 (S-99) is an inhibitor of apoptosis signal-regulated kinase 1 (ASK1) and is useful in the study of autoimmune and neurodegenerative diseases.

Aceglutamide (α-N-Acetyl-L-glutamine; N2-Acetylglutamine) (Standard) is the analytical standard of Aceglutamide (HY-B1065). This product is intended for research and analytical applications. Aceglutamide (α-N-Acetyl-L-glutamine; N2-Acetylglutamine) is a neuroprotectant that can penetrate the blood-brain barrier. Aceglutamide can enhance the antioxidant systems of glutathione (GSH), thioredoxin (Trx) and Nrf2. Aceglutamide also inhibits ASK1 and TRAF1, activates the Akt/Bcl-2 anti-apoptotic pathway, enhances the activity of antioxidant enzymes and reduces oxidative damage. Aceglutamide can improve neurological deficits after cerebral ischemia, reduce infarct volume, and inhibit neuronal apoptosis, especially substantia nigra dopaminergic neurons. Aceglutamide can reduce cerebral ischemia/reperfusion injury, improve motor dysfunction, and is used in ischemic stroke-related research.