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JNK1、JNK2和JNK3的IC50值分别为4.7 nM、18.7 nM和1 nM。
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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。 |
靶点 |
|
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]. |
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 |
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 |
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 |