ASK

NQDI 1 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50 = 3 μM, Ki = 500 nM).

Selonsertib is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.

ASK1-IN-11 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of less than 200 nM. This compound also demonstrates inhibitory effects on TNF-α, MYLK/MLCK kinases, and hERG potassium channels. The primary research applications of ASK1-IN-11 include investigations into inflammation-related pathways.

TC ASK 10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 14 nM. This compound demonstrates minimal inhibitory activity against a range of other kinases, with ASK2 being the only exception, showing an IC50 of 0.51 μM. TC ASK 10 is valuable for research applications focused on apoptosis regulation and cellular stress response pathways.

ASK1-IN-4 is a selective inhibitor of Apoptosis Signal-regulating Kinase 1 (ASK1), demonstrating an IC50 of 0.2 μM. This compound effectively interacts with the ATP-binding site of ASK1, leading to the modulation of apoptotic signaling pathways. ASK1-IN-4 is primarily utilized in research focused on apoptosis regulation, oxidative stress response, and related therapeutic investigations.

ASK1-IN-2 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), demonstrating a potent inhibitory activity with an IC50 of 32.8 nM. This compound is valuable for research applications related to ulcerative colitis, as it modulates inflammatory pathways mediated by ASK1. Its orally active nature makes it suitable for in vivo studies aimed at exploring the therapeutic potential in gastrointestinal diseases.

Selonsertib hydrochloride is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1). This compound exerts anti-inflammatory, anti-tumor, and anti-fibrotic effects by blocking the phosphorylation and activation of ASK1 through its binding to the catalytic kinase domain. It also attenuates the production of inflammatory cytokines and decreases the expression of fibrosis-related genes, thereby inhibiting excessive apoptosis and limiting cell proliferation. These properties make selonsertib hydrochloride a valuable tool for research in inflammation and fibrotic diseases.

ASK1-IN-3 is a selective inhibitor of the apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 33.8 nM. This compound demonstrates significant apoptotic induction in HepG2 cancer cells and exhibits effective cell cycle arrest. Its ability to modulate the activity of several cell cycle regulating kinases renders ASK1-IN-3 valuable for research applications related to cancer therapy and cell cycle regulation studies.

ASK1-IN-5 is a selective inhibitor of apoptosis signal-regulated kinase 1 (ASK1). This compound plays a crucial role in regulating cellular stress responses and apoptosis, making it valuable in the investigation of autoimmune and neurodegenerative diseases. Its application in research can help elucidate the mechanisms underlying these conditions and potentially guide therapeutic development.

ASK1-IN-6 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 7 nM in biochemical assays and 25 nM in cellular assays. This compound demonstrates potent anti-inflammatory properties and penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases, including Alzheimer's disease. Its specificity and efficacy position ASK1-IN-6 as a potential candidate for therapeutic exploration in related research applications.

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine is a selective inhibitor of Rho-associated protein kinase (ROCK), exhibiting IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. This compound demonstrates significant cytotoxic activity against human prostate cancer PC-3 cells, with an IC50 value of 0.16 μM. Its efficacy in inhibiting kinase activity makes it a valuable tool for research in cancer therapeutics and related signaling pathways.

MSC 2032964A is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 96 nM. This compound is shown to preserve visual responses in experimental autoimmune encephalomyelitis (EAE) mouse models and has significant efficacy in reducing neuroinflammation. Its application in research includes studies on neurodegenerative conditions and the modulation of inflammatory pathways.

GDC-3280 is an orally active anti-inflammatory and anti-fibrotic agent that operates primarily through the inhibition of the ASK1-p38 MAPK pathway. It effectively mitigates the inflammatory and fibrotic responses associated with silicosis and influences macrophage polarization. GDC-3280 is a valuable tool for research aimed at understanding and developing therapeutic strategies for inflammatory and fibrotic diseases.

ASK1-IN-1 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with a cell IC50 of 138 nM and a biochemical IC50 of 21 nM. This compound is designed to penetrate the central nervous system (CNS) and is suitable for use in research investigating the roles of ASK1 in cellular apoptosis and neurodegenerative disorders. Its inhibitory activity makes it a valuable tool for exploring therapeutic strategies targeting ASK1-related pathways.

ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications.

ASK1-IN-8 is a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. This compound demonstrates significant hepatoprotective effects in experimental models, notably reducing plasma alanine transaminase (ALT) levels in acetaminophen-induced liver injury. ASK1-IN-8 is suitable for research applications focused on liver pathologies and the modulation of apoptosis signaling pathways.

MG16 is a prodrug of 10-Methoxycamptothecin, primarily targeting CDK6 and ASK1. It effectively induces cell cycle arrest and apoptosis in cancer cells, demonstrating significant anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer. This compound is valuable for research applications focused on cancer therapeutics and the exploration of cell cycle regulation.

ASK1-IN-9 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of less than 200 nM. This compound is primarily utilized in research focused on inflammation pathways, offering insights into the role of ASK1 in cellular stress responses and programmed cell death. Its potent inhibitory effects make it a valuable tool for exploring therapeutic strategies in related diseases.

ASK1 Ligand 1 is a selective binding ligand for Apoptosis Signal-Regulating Kinase 1 (ASK1). This compound facilitates the development of PROTACs, including dASK1-VHL, enabling targeted protein degradation. Its primary applications lie in studies of apoptosis and signal transduction pathways, making it a valuable tool in cancer research and therapeutic development.

dASK1 is a selective PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1) through a cereblon (CRBN)-mediated pathway. This compound forms a stable ternary complex with ASK1, promoting its efficient degradation via the ubiquitin-proteasome system. dASK1 exhibits potent activity in degrading ASK1 and serves as a valuable tool in research focused on steatohepatitis and related pathologies.

ASK1-IN-7 is an inhibitor specifically targeting Apoptosis signal-regulating kinase 1 (ASK1). This compound is derived from a recognized ASK1 inhibitor scaffold and exhibits significant potential in modulating the ASK1 signaling pathway. Its biological activity supports research into cell stress responses, inflammation, neurodegenerative disorders, and cardiovascular diseases. ASK1-IN-7 serves as a valuable tool for understanding the role of ASK1 in various pathophysiological processes.

CS17919 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 22.52 nM. This compound demonstrates significant anti-inflammatory and antifibrotic effects, making it a valuable tool for investigating metabolic-related kidney and liver diseases. Its oral bioavailability enhances its utility in preclinical studies aimed at understanding ASK1's role in disease mechanisms and potential therapeutic interventions.

DDO3711 is a specific inhibitor of apoptosis signal-regulated kinase 1 (ASK1), exhibiting an IC50 of 164.1 nM while displaying minimal inhibition of ASK2 (IC50 > 20 μM). This compound functions by dephosphorylating phosphorylated ASK1 at threonine 838 through recruitment of the phosphatase PP5. DDO3711 demonstrates significant ASK1-dependent antiproliferative effects and shows promise in studies related to cancer by targeting abnormally phosphorylated oncoproteins.

JT21-25 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 5.1 nM. This compound plays a crucial role in inhibiting apoptotic signaling pathways, making it valuable for research focused on cellular stress responses and apoptosis. JT21-25 is utilized in studies investigating the modulation of ASK1 activity in various disease models, particularly those related to neurodegenerative disorders and cancer.