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JNK-IN-8 Sale

(Synonyms: JNK Inhibitor XVI) 目录号 : GC13841

JNK-IN-8 是第一个不可逆的JNK抑制剂,作用于JNK1,JNK2和JNK3,在A375细胞系中IC50分别为4.7 nM,18.7 nM和1 nM。

JNK-IN-8 Chemical Structure

Cas No.:1410880-22-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥774.00
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2mg
¥434.00
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5mg
¥693.00
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10mg
¥1,246.00
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50mg
¥3,920.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

HEK293-ILR1、A375 cells

Preparation Method

The cells were incubated with JNK-IN-8 at concentrations of 0.1, 0.3, 1, and 3 µM for 3 h.

Reaction Conditions

0.1, 0.3, 1, 3 µM ; 3 h

Applications

The superior potency and selectivity of JNK-IN-8 in the HEK293 cells suggested that the compound would likely serve as very useful pharmacological probes of JNK-dependent cellular phenomena.

Animal experiment [2]:

Animal models

SD rats

Preparation Method

Rats were given an intraperitoneal injection of vehicle (saline 150 δl and 20% dimethylsulfoxide in PBS) or JNK-IN-8 (20 mg/kg dissolved in 20% dimethylsulfoxide) after MCAO.

Dosage form

20 mg/kg; i.p.

Applications

JNK-IN-8-treated rats with MCAO exerted a significant improvement in spatial learning as measured by the improved mNSS, and showed sensorimotor functional recovery as measured by the Foot-fault test.

References:

[1]Zhang T, Inesta-Vaquera F, et al, Discovery of potent and selective covalent inhibitors of JNK. Chemical Biology. 2012, 19(1):140-154.
[2] Geng W , Tang H , Dai Q ,et al. JNK-IN-8, a c-Jun N-terminal kinase inhibitor, improves functional recovery through suppressing neuroinflammation in ischemic stroke[J].Cold Spring Harbor Laboratory, 2018.

产品描述

JNK-IN-8 is the first irreversible JNK inhibitor that acts on JNK1, JNK2, and JNK3 with high specificity, with IC50 values of 4.7 nM, 18.7 nM, and 1 nM in the A375 cell line, respectively[1]. JNK-IN-8 forms a covalent bond with the conserved cysteine residue of JNK 1/2/3, causing a conformational change in the activation loop and blocking substrate binding, thereby inhibiting the activity of JNK 1/2/3[1]. JNK 1, 2, and 3 are part of the mitogen-activated protein kinase (MAPK) family, capable of phosphorylating the Ser 63 and Ser 73 residues of c-Jun, responding to stress stimuli such as cytokines and heat shock, and involved in T cell differentiation and apoptosis processes.

In vitro, JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells, with EC50 values of 486 nM and 338 nM, respectively[1]. JNK-IN-8 also shows significant selectivity in HEK 293 cells[1]. Additionally, JNK-IN-8 (10 mM) exhibits anti-inflammatory effects, reducing microglial activation and the expression of IL-6, IL-1β, and TNF-α[2].

In vivo, JNK-IN-8 (20 mg/kg; i.p.) treated rats with middle cerebral artery occlusion show significant improvements in spatial learning and sensorimotor function recovery[2]. Administration of JNK-IN-8 (3µg/µL) into the lateral ventricles of male KM mice 24 h before brain injury significantly reduces neuronal apoptosis after brain injury[3].

References:
[1] Zhang T, Inesta-Vaquera F, et al, Discovery of potent and selective covalent inhibitors of JNK. Chemical Biology. 2012, 19(1):140-154.
[2] Geng W , Tang H , Dai Q ,et al. JNK-IN-8, a c-Jun N-terminal kinase inhibitor, improves functional recovery through suppressing neuroinflammation in ischemic stroke[J].Cold Spring Harbor Laboratory, 2018.
[3] Li D1, Liu N, et al, Protective effect of resveratrol against nigrostriatal pathway injury in striatum via JNK pathway. Brain Res. 2017 Jan 1;1654(Pt A):1-8.

JNK-IN-8 是第一个不可逆的JNK抑制剂,作用于JNK1,JNK2和JNK3,具有高度特异性,在A375细胞系中IC50分别为4.7 nM,18.7 nM和1 nM[1]。JNK-IN-8与JNK 1/2/3的保守半胱氨酸残基形成共价键,导致激活环的构象变化,阻断底物结合,从而抑制JNK 1/2/3的活性[1]。JNK 1、2和3属于丝裂原活化蛋白激酶(mitogen-activated protein kinase,MAPK)家族,能够磷酸化c-Jun的Ser 63和Ser 73残基,对细胞因子和热休克等应激刺激有应答,参与T细胞分化和细胞凋亡过程。

在体外,JNK-IN-8 抑制 HeLa和A375细胞中的c-Jun磷酸化,EC50分别为 486 nM和338 nM[1]。JNK-IN-8在HEK 293细胞中还表现出显著的选择性[1]。JNK-IN-8 (10 mM)还发挥抗炎作用,使小胶质细胞活化减少以及 IL-6、IL-1β和TNF-α 表达减少[2]

在体内,JNK-IN-8 (20 mg/kg; i.p.)治疗的大脑中动脉闭塞大鼠在空间学习方面表现出显着改善,并且感觉运动功能恢复[2]。JNK-IN-8在雄性KM小鼠脑损伤前24 h向侧脑室注射3µg/µL 能显著减少脑损伤后神经元凋亡[3]

Chemical Properties

Cas No. 1410880-22-6 SDF
别名 JNK Inhibitor XVI
化学名 3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[3-methyl-4-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
Canonical SMILES CC1=C(C=CC(=C1)NC(=O)C2=CC(=CC=C2)NC(=O)C=CCN(C)C)NC3=NC=CC(=N3)C4=CN=CC=C4
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 储存条件 Store at -20°C
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1 mM 1.9701 mL 9.8505 mL 19.7009 mL
5 mM 0.394 mL 1.9701 mL 3.9402 mL
10 mM 0.197 mL 0.985 mL 1.9701 mL
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