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JNK-IN-7 {[allProObj[0].p_purity_real_show]}

货号:A537026 同义名: JNK inhibitor;JNK Inhibitor VII

JNK-IN-7 is a potent inhibitor for JNK all isoforms with IC50 values of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.

JNK-IN-7 化学结构 CAS号:1408064-71-0
JNK-IN-7 化学结构
CAS号:1408064-71-0
JNK-IN-7 3D分子结构
CAS号:1408064-71-0
JNK-IN-7 化学结构 CAS号:1408064-71-0
JNK-IN-7 3D分子结构 CAS号:1408064-71-0
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JNK-IN-7 纯度/质量文件 产品仅供科研

货号:A537026 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 JNK JNK1 JNK2 JNK3 其他靶点 纯度
Mulberroside A 99%+
Loureirin B Potassium Channel,Calcium Channel 99%+
Ginsenoside Re NF-κB 98%
(+)-(3R,8S)-Falcarindiol STAT,ERK 99%+
trans-Zeatin ERK,p38 MAPK 95+%
Urolithin B ERK,NF-κB 95%
Cucurbitacin IIb NF-κB 98+%
Astragaloside IV mTOR,NF-κB,Akt 98%
NDMC101 99%+
DB07268 ++++

JNK1, IC50: 9 nM

99%+
SP600125 +

MKK4, IC50: 0.4 μM

+++

JNK1, IC50: 40 nM

+++

JNK2, IC50: 40 nM

+++

JNK3, IC50: 90 nM

98%
JNK-IN-7 ++++

JNK1, IC50: 1.5 nM

++++

JNK2, IC50: 2 nM

++++

JNK3, IC50: 0.7 nM

98+%
JNK-IN-8 ++++

JNK1, IC50: 4.7 nM

+++

JNK2, IC50: 18.7 nM

++++

JNK3, IC50: 1 nM

99%+
3,3',5-Triiodo-L-thyronine ++

JNK1, Kd: 240 nM

++

JNK2, Kd: 290 nM

+++

JNK3, Kd: 66 nM

98%
IQ-1S free acid +

JNK1, IC50: 390 nM

++

JNK2, IC50: 360 nM

+++

JNK3, IC50: 87 nM

98%
BI-78D3 ++

JNK, IC50: 280 nM

++

JNK, IC50: 280 nM

++

JNK, IC50: 280 nM

++

JNK, IC50: 280 nM

99%+
Bentamapimod +++

JNK1, IC50: 80 nM

+++

JNK2, IC50: 90 nM

++

JNK3, IC50: 230 nM

98%
Resveratrol +

JNK1, IC50: 50 μM

98%
Indirubin-3′-oxime 99%+
SU3327 +

JNK, IC50: 0.7 μM

+

JNK, IC50: 0.7 μM

+

JNK, IC50: 0.7 μM

+

JNK, IC50: 0.7 μM

99%+
JNK Inhibitor VIII ++++

JNK1, Ki: 2 nM

JNK1, IC50: 45 nM

++++

JNK2, IC50: 160 nM

JNK2, Ki: 4 nM

+++

JNK3, Ki: 52 nM

98%
Doramapimod 99%+
RPI-1 97%
TCS JNK 5a ++

JNK2, pIC50: 6.5

++

JNK3, pIC50: 6.7

98%
SP 600125, negative control +

JNK2, IC50: 18 μM

+

JNK3, IC50: 24 μM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

JNK-IN-7 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].

JNK-IN-7 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.

JNK-IN-7 实验方案

计算器
存储液制备 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

JNK-IN-7 技术信息

CAS号1408064-71-0
分子式C28H27N7O2
分子量 493.56
别名 JNK inhibitor;JNK Inhibitor VII;c-Jun N-terminal Kinase Inhibitor VII
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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