175026-96-7

Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death. NQDI-1 is a specific inhibitor of ASK1 (IC₅₀ = 3 μM; K_i = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases. It has been used to promote survival of induced pluripotent stem cell populations and to protect neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

NQDI-1 is an ASK1 inhibitor which is of therapeutic potential against acute ischemic renal injury. ?Its protective effects are mediated through inhibition of apoptosis and oxidative stress.

ASK1: 500 nM (Ki); ASK1: 3 μM (IC₅₀)

Volynets et al. (2011), Identification of 2H-naphtho[1,2,3-de]quinoline-2,7-diones as inhibitors of apoptosis signal-regulating kinase 1 (ASK1); Med. Chem., 54 2680 Nomura et al. (2013), An ASK1-p38 signaling pathway mediates hydrogen peroxide-induced toxicity in NG108-15 neuronal cells; Lett., 549 163 Chen et al. (2019), The MC4 receptor agonist RO27-3225 inhibits NLRP1-dependent neuronal pyroptosis via the ASK1/JNK/p38 MAPK pathway in a mouse model of intracerebral haemorrhage; J. Pharmacol., 176 1341 Ma et al. (2019), Low glucose and metformin-induced apoptosis of human ovarian cancer cells is connected to ASK1 via mitochondrial and endoplasmic reticulum stress associated pathways; Exp. Clin. Cancer Res., 38 77 Feng et al. (2018), Dual function of peroxiredoxin I in lipopolysaccharide-induced osteoblast apoptosis via reactive oxygen species and the apoptosis signal-regulating kinase 1 signaling pathway; Cell Death Discov., 4 47