ask1

ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.

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].

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.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

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

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

GS-444217 is a selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50: 2.87 nM).

ASK1ligand 1 is a binding ligand for ASK1 and can be utilized to synthesize PROTACs such as dASK1-VHL.

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. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.

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-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-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.

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. It effectively binds to VHL, promoting the selective degradation of ASK1. By reducing ASK1 protein levels, dASK1-VHL inhibits the activation of p38 MAPK and decreases liver lipid content, offering new insights for MASH research.

dASK1 is a selective CRBN-based PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1). It forms a stable ternary complex with ASK1, facilitating its rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 exhibits strong ASK1 degradation capabilities and is applicable for hepatitis research.

AVE1231 is a TASK-1 channel blocker that inhibits TASK-1 and can be used in the study of atrial fibrillation.

A2793 is a dual inhibitor of TWIK-associated acid-sensitive K+ channel 1 (TASK-1)/TRESK, with an IC50 for mTRESK of 6.8 μM. It is more selective for TRESK, and relatively weaker for TREK-1 and TALK-1.

JT21-25 (compound 9h) acts as a potent, selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of 5.1 nM [1].

Doxapram hydrochloride hydrate (Doxapram HCl) effectively inhibits the function of TASK-1, TASK-3, and TASK-1/TASK-3 heterodimeric channels, displaying EC50 values of 410 nM, 37 μM, and 9 μM, respectively.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

Doxapram (Dopram) is a respiratory stimulant that inhibits TASK-1, TASK-3, and TASK-1/TASK-3 heterodimer channels and is used to study ventilatory failure caused by apnea of ​​prematurity and exacerbation of chronic obstructive pulmonary disease.

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

Limertinib (ASK120067) is an orally active and highly efficient epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor targeting EGFR T790M. Limertinib can be used for studying non-small cell lung cancer.

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).