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JNK-IN-8 {[allProObj[0].p_purity_real_show]}

货号:A206353 同义名: JNK Inhibitor XVI;c-Jun N-terminal Kinase Inhibitor XVI

JNK-IN-8是一种高效的JNK抑制剂,对JNK1JNK2JNK3IC50值分别为4.7 nM、18.7 nM和1 nM。

JNK-IN-8 化学结构 CAS号:1410880-22-6
JNK-IN-8 化学结构
CAS号:1410880-22-6
JNK-IN-8 3D分子结构
CAS号:1410880-22-6
JNK-IN-8 化学结构 CAS号:1410880-22-6
JNK-IN-8 3D分子结构 CAS号:1410880-22-6
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JNK-IN-8 纯度/质量文件 产品仅供科研

货号:A206353 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 NF-κB,ERK 95%
Cucurbitacin IIb NF-κB 98+%
Astragaloside IV NF-κB,Akt,mTOR 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-8 生物活性

靶点
  • JNK1

    JNK1, IC50:4.7 nM

  • JNK2

    JNK2, IC50:18.7 nM

  • JNK3

    JNK3, IC50:1 nM

描述 c-Jun N-terminal kinases (JNK1/2/3) are key enzymes in the inflammatory signaling network. JNK-IN-8 is a covalent JNK inhibitor with IC50 values of 4.67, 18.7, and 0.98 nM for JNK1, JNK2, and JNK3, respectively. The EC50 values of JNK-IN-8 for the inhibition of c-Jun phosphorylation in Hela and A375 cells are 486 and 338 nM, respectively. JNK-IN-8 possessed a selective S (10) score of 0.031[3]. In P411-T1 patient-derived xenograft-derived cells, treatment with 1μM JNK-IN-8 for 24 h led to a significant decrease in p-JUN. JNK-IN-8 at 1 μM also enhanced the inhibitory effect of FOLFOX chemotherapy on cell growth and reversed FOLFOX-induced JUN activation in P441-T1, P442-T1, CFPAC-1, and MIA PaCa-2 cells. In mice bearing pancreatic ductal adenocarcinoma tumors, JNK-IN-8 (30 mg/kg, 2×/week) enhanced the efficacy of FOLFOX chemotherapy on tumor growth[4].
作用机制 JNK-IN-8 inhibits the kinase activity of JNK through the medication of a conserved cysteine in its ATP-binding motif[3].

JNK-IN-8 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A375 cells Function assay 1 h Inhibition of JNK3-mediated c-jun phosphorylation in human A375 cells after 1 hr incubation, IC50=0.338 μM 25415535
human HeLa cells Function assay 1 h Inhibition of JNK3-mediated c-jun phosphorylation in human HeLa cells after 1 hr incubation, IC50=0.486 μM 25415535

JNK-IN-8 参考文献

[1]19(1):140-154. doi:10.1016/j.chembiol.2011.11.010

[2]5(8):e129905. doi:10.1172/jci.insight.129905

JNK-IN-8 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL

JNK-IN-8 技术信息

CAS号1410880-22-6
分子式C29H29N7O2
分子量 507.586
别名 JNK Inhibitor XVI;c-Jun N-terminal Kinase Inhibitor XVI
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,Inert atmosphere,2-8°C

溶解度

DMSO: 35 mg/mL(68.95 mM),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

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

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