NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM.
NQDI-1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BV-2 cells
10 μM
24 h
NQDI1 decreased the phosphorylation and expression of ASK1, reduced the phosphorylation of p-38 and JNK, decreased the activity and the expression of MMP-9, and inhibited IBA-1 expression.
J Neuroinflammation. 2023 Feb 3;20(1):22.
SKOV3 cells
10 μM
24 h
Inhibition of ASK1 expression, reduction of total Noxa protein and mitochondrial localization, and increase in Bcl-2 expression, thereby attenuating low glucose and metformin-induced apoptosis
J Exp Clin Cancer Res. 2019 Feb 13;38(1):77.
mouse embryonic fibroblasts (MEFs)
10 μM, 30 μM, 50 μM
24 h
To determine the inhibitory effect of NQDI-1 on ASK1 phosphorylation, results showed that 10 μM NQDI-1 reduced ASK1 phosphorylation to 40% of control, 30 μM almost completely inhibited, and 50 μM completely inhibited ASK1, JNK, and p38 phosphorylation.
Cell Death Dis. 2014 Nov 13;5(11):e1522.
NQDI-1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Postoperative pain model
Intrathecal injection
5 μg/10 μl
Once daily for 5 days
NQDI-1 decreased the phosphorylation of ASK1, p-38, and JNK, reduced the activity and expression of MMP-9, and attenuated postoperative pain.
J Neuroinflammation. 2023 Feb 3;20(1):22.
Nude mice
Ovarian cancer xenograft model
Intraperitoneal injection
1 mg/kg
Once daily until tumor volume reached 150-200 mm3
To evaluate the inhibitory effect of NQDI-1 on the anti-tumor activity of metformin, it was found that NQDI-1 weakened the anti-tumor effect of metformin alone
J Exp Clin Cancer Res. 2019 Feb 13;38(1):77.
Mice
Ectopic ossification model
Subcutaneous injection
30 μM
Single injection, lasting 2 weeks
To evaluate the effect of NQDI-1 on ectopic ossification, results showed that 30 μM NQDI-1 increased bone volume by 64%, comparable to the 82% increase observed in ASK1 KO mice.
Cell Death Dis. 2014 Nov 13;5(11):e1522.
Mice
Intracerebral hemorrhage model
Intracerebroventricular injection
250 nM/mouse
Single dose 30 min before ICH induction
NQDI-1 alone improved neurological functions and down-regulated ASK1/JNK/p38 MAPK expression after ICH.
Br J Pharmacol. 2019 May;176(9):1341-1356
Mice
Liver ischemia/reperfusion injury model
Intraperitoneal injection
10 mg/kg
Single injection, lasting until 6 hours after reperfusion
NQDI-1 alleviates liver ischemia/reperfusion injury by inhibiting the ASK1-JNK/P38 signaling pathway
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