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[CAS NO. 175026-96-7] NQDI-1
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-19566 |
| Brand: | MCE |
| CAS: | 175026-96-7 |
Overview
| MDL | MFCD03265970 |
|---|---|
| Molecular Weight | 319.31 |
| Molecular Formula | C19H13NO4 |
| SMILES | O=C(C1=C2C3=C(NC1=O)C=CC=C3C(C4=C2C=CC=C4)=O)OCC |
5 Publications Citing Use of MCE
Summary
NQDI-1 inhibits apoptosis signal-regulating kinase 1 ( ASK1 ) with a K i of 500 nM and an IC 50 of 3 μM.
IC50 & Target
|
ASK1 3 μM (IC 50 ) |
In Vitro
The selectivity of NQDI-1 is evaluated in vitro on four serine/threonine protein kinases (protein kinase CK2 (CK2), c-Jun N-terminal kinase 3 (JNK3), Rho-associated protein kinase 1 (Rock1), and Aurora A) and three tyrosine protein kinases (FGFR1, hHGFR, and endothelial TEK tyrosine kinase (Tie2)). The results show that NQDI-1 is a selective inhibitor of ASK1. The activity of FGFR1 protein kinase is inhibited by NQDI-1 (residual activity of 44%). NQDI-1 inhibits ASK1 with a K i of 500 nM. Inhibition of ASK1 by NQDI-1 is competitive with respect to the phosphodonor substrate ATP [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
250 nmol NQDI-1 in DMSO is intracerebroventricularly injected following brain insult. Western blotting is performed to determine the expression of ASK1 in the sham, Hypoxia-ischemia (HI), DMSO and NQDI-1 groups and indicate that NQDI-1 markedly inhibits the expression of ASK1 in the brain cortex, compared with the HI and DMSO group. Furthermore, immunofluorescence staining also indicates that the expression of ASK1 is inhibited by NQDI-1 in the brain cortex. The expression of downstream targets of ASK1 is also determined in the present study. The expression levels of p-JNK, p-c-Jun, p53 and caspase 3 are significantly decreased by NQDI-1, compared with the HI and DMSO groups. Low expression of p-JNK in the brain cortex is also observed by immunofluorescence in the NQDI-1-treated group [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 10 mg/mL ( 31.32 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1318 mL | 15.6588 mL | 31.3175 mL |
| 5 mM | 0.6264 mL | 3.1318 mL | 6.2635 mL |
| 10 mM | 0.3132 mL | 1.5659 mL | 3.1318 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 0.71 mg/mL (2.22 mM); Suspended solution; Need ultrasonic
References
- [1] Volynets GP, et al. Identification of 3H-naphtho[1,2,3-de]quinoline-2,7-diones as inhibitors of apoptosis signal-regulating kinase 1 (ASK1). J Med Chem. 2011 Apr 28;54(8):2680-6.
- [2] Hao H, et al. NQDI-1, an inhibitor of ASK1 attenuates acute perinatal hypoxic-ischemic cerebral injury by modulating cell death. Mol Med Rep. 2016 Jun;13(6):4585-92.
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