JNK Inhibitor VIII

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Chemical Structure| 894804-07-0 同义名 : TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII;TCS JNK 6o
CAS号 : 894804-07-0
货号 : A872802
分子式 : C18H20N4O4
纯度 : 98%
分子量 : 356.376
MDL号 : MFCD19690908
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
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：
生物活性
靶点

  • JNK1

    JNK1, Ki:2 nM

    JNK1, IC50:45 nM

  • JNK2

    JNK2, IC50:160 nM

    JNK2, Ki:4 nM

  • JNK3

    JNK3, Ki:52 nM
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].
实验方案
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
参考文献

[1]Szczepankiewicz BG, et al. Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006 Jun 15;49(12):3563-80.

[2]Szczepankiewicz BG, Kosogof C, Nelson LT, et al. Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006;49(12):3563-3580

[3]Bertoldo MJ, Bernard J, Duffard N, et al. Inhibitors of c-Jun phosphorylation impede ovine primordial follicle activation. Mol Hum Reprod. 2016;22(5):338-349