ASK1

Apoptosis signal-regulating kinase 1; MAP3K5; MAPKKK5; Mitogen-activated protein kinase kinase kinase 5; MEK kinase 5

Apoptosis signal-regulating kinase 1 (ASK1) is a member of the mitogen-activated protein kinase (MAP3K) family which acts as an upstream regulator for the activation of p38 MAPK and c-Jun N-terminal kinase (JNK). Under normal physiological conditions, ASK1 is maintained in an inactive state through binding to the reduced form of thioredoxin. However, during pathological conditions which induce intracellular production of reactive oxygen species (e.g., mitochondrial or endoplasmic reticulum stress), thioredoxin is oxidized and dissociates from ASK1 facilitating activation of ASK1 and downstream p38 MAPK and JNK signaling that can cause tissue injury .

ASK1 Related Products (24):

By Effects:	Inhibitors (16) Agonists (2) Degraders (3) Ligand (1) Activators (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-B1065

Aceglutamide	Inhibitor	98.0%
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.

HY-N1508

Ecliptasaponin A	Agonist	99.81%
Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.

HY-131969

ASK1-IN-2	Inhibitor	99.37%
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.

HY-160939

ASK1-IN-6	Inhibitor	98.13%
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.

HY-160851

GDC-3280	Inhibitor	98.82%
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.

HY-183960

BPyO-34	Inhibitor
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.

HY-183766

HYF038	Ligand
HYF038 is a blood-brain barrier-penetrant ligand of apoptosis signal-regulating kinase 1 (ASK1). When labeled with ¹¹C, HYF038 can be used for ASK1 neuroimaging studies.

HY-182071

MG16	Activator
MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer.

HY-133554

ASK1-IN-1	Inhibitor	98.74%
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).

HY-153761

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

HY-179033

Nur77 antagonist 2	Activator
Nur77 antagonist 2 (Compound 12b) is an orally active Nur77 antagonist with a K_D value of 0.42 μM. Nur77 antagonist 2 exhibits proliferative activity on liver cancer cells. Nur77 antagonist 2 stabilizes Nur77 by inhibiting its ubiquitin-proteasomal degradation, leading to Nur77-dependent apoptosis via the ASK1-JNK/p38 pathway. Nur77 antagonist 2 inhibits tumor growth in the HCCLM3 xenograft model. Nur77 antagonist 2 can be used for the study of hepatocellular carcinoma (HCC).

HY-176881

ASK1-IN-10	Inhibitor
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.

HY-173293

ASK1-IN-8	Inhibitor
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.

HY-176882

ASK1-IN-11	Inhibitor
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.

HY-176880

ASK1-IN-9	Inhibitor
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.

HY-174858

dASK1-VHL	Degrader
dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861).

HY-146729

ASK1-IN-3	Inhibitor
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.

HY-179517

ASK1-IN-12	Inhibitor
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).

HY-174860

ASK1 ligand 1	Degrader
ASK1 ligand 1 is a binding ligand for ASK1 and can be used to synthesize PROTACs such as dASK1-VHL (HY-174858^)[1].

HY-174862

dASK1	Degrader
dASK1 is a selective and cereblon (CRBN)-based PROTAC degrader of apoptosis signal-regulating kinase 1 (ASK1). dASK1 forms a stable ternary complex with ASK1, facilitating ASK1 rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 demonstrates potent ASK1 degradation. dASK1 can be used for the research of steatohepatitis. (Structure Note: Pink: ASK1 ligand (HY-174860); Blue: CRBN ligand (HY-10984); Black: linker; E3-linker (HY-174863))

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