ask1

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

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.

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

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.

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].

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

Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).

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.

(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde (MDA) and decreases in superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities as well as increases constitutive nitric oxide synthase (cNOS) activity and nitric oxide (NO) production in HUVECs. CSTMP also induces cell death of A549 non-small cell lung cancer (NSCLC) cells in an IRE1α-dependent manner through induction of IRE1α-TRAF2-ASK1 complex-mediated endoplasmic reticulum (ER) stress and mitochondrial apoptosis.

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

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.

K812 is an ASK1-specific inhibitor discovered to prolong survival in a mouse model of amyotrophic lateral sclerosis.

K811 is an ASK1-specific inhibitor that prolongs survival in a mouse model of amyotrophic lateral sclerosis. K811 efficiently prevented cell proliferation in cell lines with high ASK1 expression and in HER2-overexpressing GC cells. Treatment with K811 reduced sizes of xenograft tumors by downregulating proliferation markers.

DDO3711, a PP5-recruiting phosphatase recruitment chimera (PHORC), is created by chemically linking an apoptosis signal-regulated kinase 1 (ASK1) inhibitor with a PP5 activator. This compound selectively targets ASK1 (IC50=164.1 nM) over ASK2 (IC50 >20 μM), effectively dephosphorylating p-ASK1 T838 through PP5 recruitment. Exhibiting ASK1-dependent antiproliferative properties, DDO3711 demonstrates anti-cancer activity, making it a promising agent for research into the abnormal phosphorylation of oncoproteins.

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].

Sulfotanshinone IIA Sodium mitigates oxidative damage in peritoneal mesothelial cells caused by peritoneal dialysis solution (PDS) by inhibiting the ASK1-p38 signaling pathway.

Compound 7, also known as 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine, serves as an inhibitor of protein kinases, displaying IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. Additionally, this compound exhibits significant cytotoxicity towards PC-3 cancer cells, with an IC50 of 0.16 μM [1].

Antagonist of 14.3.3 proteins (KD ≈80 nM). Competitively inhibits 14.3.3-ligand interactions without requiring phosphorylation. Blocks the ability of 14.3.3 to bind to target proteins such as Raf-1, Bad, ASK1 and exoenzyme S.