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NQDI-1

目录号: PL06936 纯度: ≥98%

NQDI-1 抑制凋亡信号调节激酶 1 (ASK1)，Ki 为 500 nM，IC50 为 3 μM。

CAS No. :175026-96-7

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中文名称	NQDI-1
中文别名	2,7-二氢-2,7-二氧代-3H-萘并[1,2,3-DE]喹啉-1-羧酸乙酯;NQDI1 抑制剂;LESINURAD (RDEA-594)中间体;LESINURAD (RDEA-594)中间体LESINURAD (RDEA-594) INTERMEDIATE
英文名称	NQDI-1
英文别名	NQDI 1;NQDI-1;Ethyl 2,7-dioxo-2,7-dihydro-3H-naphtho[1,2,3-de]quinoline-1-carbo xylate;NDQI 1;LESINURAD (RDEA-594) intermediate;2,7-Dihydro-2,7-dioxo-3H-naphtho[1,2,3-de]quinoline-1-carboxylic acid ethyl ester;3H-Naphtho[1,2,3-de]quinoline-1-carboxylic acid, 2,7-dihydro-2,7-dioxo-, ethyl ester;MLS000715851;SMR000277368;ethyl 2,7-dioxo-3,7-dihydro-2H-naphtho[1,2,3-de]quinoline-1-carboxylate;ethyl 2,7-dioxo-2,7-dihydro-3H-naphtho[1,2,3-de]quinoline-1-carboxylate;BAS 05532741;Oprea1_559557;Oprea1_384256;IFLab1_005737;cid_5522952;BDBM32315;HMS2646I12;HMS1428E17;BCP16684;s8289;STL514199;STK793109;Ethyl 8,15-dioxo-14-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2,4,6,9(17),10,12-heptaene-16-ca
Cas No.	175026-96-7
分子式	C₁₉H₁₃NO₄
分子量	319.31
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	NQDI-1 抑制凋亡信号调节激酶 1 (ASK1)，Ki 为 500 nM，IC50 为 3 μM。

产品详情	NQDI-1 抑制凋亡信号调节激酶 1 (ASK1)，K_i 为 500 nM，IC₅₀ 为 3 μM。
生物活性	NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a K i of 500 nM and an IC 50 of 3 μM.
性状	Solid
IC50 & Target[1][2]	ASK1 3 μM (IC50)
体外研究(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 Ki of 500 nM. Inhibition of ASK1 by NQDI-1 is competitive with respect to the phosphodonor substrate ATP. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed th
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 10 mg/mL (31.32 mM; Need ultrasonic and warming)配制储备液

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[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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