產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg
CAS	1410880-22-6
別名
化學(xué)名	3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[3-methyl-4-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
分子式	C29H29N7O2
分子量	507.59
溶解度	≥ 25.4 mg/mL in DMSO, ≥ 9.24 mg/mL in EtOH with ultrasonic and warming
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

JNK-IN-8 is a specific JNK1/2/3 inhibitor with IC50 value of 4.67, 18.7, 0.98 nM respectively [1].

C-Jun N-terminal kinase (JNK) 1, 2 and 3 belong to the mitogen-activated protein kinase (MAPK) family, which are able to phosphorylate c-Jun on the Ser63 and Ser73 residue.They are responsive for stress stimuli, including cytokines and heat shock, and get involved in T cell differentiation and cell apoptosis process. JNK 1 and 2 are ubiquitous in all cell types but JNK 3 is only found in cells of brain, heart and testes tissues.

JNK-IN-8 is a JNK1/2/3 inhibitor with high specificity. When JNK-IN-8 was profiled with a panel of 400 kinases, it exhibited specific binding to JNK 1/2/3 but not to other kinases. Crystallization study also found that JNK-IN-8 forms covalent bonds with conserved cysteine residue of JNK 1/2/3, resulting in a conformational change of the activation loop that blocks the substrate binding, thereby inhibiting the activity of JNK 1/2/3 [1].

In Hela cells and A375 cells, pretreatment of cells with JNK-IN-8 resulted in the inhibition of c-Jun which is a direct phosphorylation substrate of JNK 1/2/3, confirming the inhibitory action of JNK-IN-8 on JNK 1/2/3. In HEK293-ILR1 cells following stimulation by anisomycin, the JNK-IN-8 was observed to inhibit c-Jun but not MSK1 and p38, and the inhibition was not reversible by removing JNK-IN-8 from culture medium. Additionally, JNK-IN-8 only exhibited on-pathway inhibition of JNK signaling pathway, which can be monitored by the phosphorylation of c-Jun [1].

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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