产品说明书

JNK-IN-7

Print
Chemical Structure| 1408064-71-0 同义名 : JNK inhibitor;JNK Inhibitor VII;c-Jun N-terminal Kinase Inhibitor VII
CAS号 : 1408064-71-0
货号 : A537026
分子式 : C28H27N7O2
纯度 : 98+%
分子量 : 493.56
MDL号 : MFCD25976765
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(70.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JNK1

    JNK1, IC50:1.5 nM

  • JNK2

    JNK2, IC50:2 nM

  • JNK3

    JNK3, IC50:0.7 nM
描述 JNKs (c-jun NH2-terminal kinases) are serine/threonine-protein kinase involved in various processes such as cell proliferation, differentiation, migration, transformation and programmed cell death. Extracellular stimuli such as proinflammatory cytokines or physical stress stimulate the JNK signaling pathway. There are three distinct alternatively spliced genes (Jnk1, Jnk2, and Jnk3) that produce approximately ten different proteins. The predominant isoforms JNK1 and JNK2 are ubiquitously expressed, but JNK3 is expressed primarily in the nervous system. JNK-IN-7 is a JNK inhibitor with IC50 values of 1.54 nM, 1.99 nM, 0.75 nM to JNK1, JNK2, JNK3, respectively[3]. It also inhibits phosphorylation of c-Jun, which is a direct substrate of JNK kinase in Hela and A375 cells, with EC50s of 130nM and 244nM, respectively[3]. At the concentration of 1μM, 48h incubation of JNK-IN-7 could rescue the down-regulation of DMT-1 expression resulted by TNF[4]. At the concentrations of 1mM or 10mM, JNK-IN-7 inhibited the IL-1-stimulated activation of Pellino 1 in IL-1R cells[5].
作用机制 JNK-IN-7 is a covalent inhibitor of JNKs[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.26mL

4.05mL

2.03mL
参考文献

[1]Wu W, Song Y, et al. Divalent metal-ion transporter 1 is decreased in intestinal epithelial cells and contributes to the anemia in inflammatory bowel disease. Sci Rep. 2015 Nov 17;5:16344.

[2]Zhang T, Inesta-Vaquera F, et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54.

[3]Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54.

[4]Wu W, Song Y, He C, Liu C, Wu R, Fang L, Cong Y, Miao Y, Liu Z. Divalent metal-ion transporter 1 is decreased in intestinal epithelial cells and contributes to the anemia in inflammatory bowel disease. Sci Rep. 2015 Nov 17;5:16344.

[5]Goh ET, Arthur JS, Cheung PC, Akira S, Toth R, Cohen P. Identification of the protein kinases that activate the E3 ubiquitin ligase Pellino 1 in the innate immune system. Biochem J. 2012 Jan 1;441(1):339-46.