货号:A872802 同义名: TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII
JNK Inhibitor VIII是一种c-Jun氨基末端激酶(JNK-1、-2、-3)抑制剂,Ki值分别为2 nM、4 nM和52 nM,IC50值分别为45 nM和160 nM(针对JNK-1和JNK-2)。
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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 | ✔ | ERK,STAT | 99%+ | ||||||||||||||||
trans-Zeatin | ✔ | ERK,p38 MAPK | 95+% | ||||||||||||||||
Urolithin B | ✔ | ERK,NF-κB | 95% | ||||||||||||||||
Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
Astragaloside IV | ✔ | Akt,mTOR,NF-κB | 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 |
99% | |||||||||||||||
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 |
99% | |||||||||||||||
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, IC50: 45 nM JNK1, Ki: 2 nM |
++++
JNK2, Ki: 4 nM JNK2, IC50: 160 nM |
+++
JNK3, Ki: 52 nM |
98% | |||||||||||||||
Doramapimod | ✔ | 99%+ | |||||||||||||||||
RPI-1 | ✔ | 99% | |||||||||||||||||
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 kinase-1 (JNK-1) is a member of the mitogen activated protein kinase (MAP kinase) family of enzymes responsible for the serine/threonine phosphorylation of intracellular targets. JNK-1 and the other JNK enzymes JNK-2 and JNK-3 are activated in response to cellular stresses and various cytokines, and they participate in the onset of apoptosis. TCS JNK 6o is a pan-JNK inhibitor with Ki values of 2, 4 and 52 nM for JNK-1, JNK-2 and JNK-3, respectively, and has IC50 values of 45 and 160 nM for JNK-1 and JNK-2, respectively. In Sprague-Dawley rats, TCS JNK 6o showed a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism was very rapid with this compound[2]. Moreover, inhibition of primordial follicle activation occurred in the presence of TCS JNK 6o when compared with controls (P < 0.05) after 2 days of culture[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.03mL 2.81mL 1.40mL |
28.06mL 5.61mL 2.81mL |
CAS号 | 894804-07-0 |
分子式 | C18H20N4O4 |
分子量 | 356.376 |
别名 | TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII;TCS JNK 6o |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 250 mg/mL(701.51 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 |