TCS JNK 5a

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Chemical Structure| 312917-14-9 同义名 : JNK Inhibitor IX; c-Jun N-terminal Kinase Inhibitor IX; TCS JNK 5a, TCS-JNK-5a, JNK Inhibitor IX, SC-202671, SC 202671, SC202671
CAS号 : 312917-14-9
货号 : A222483
分子式 : C20H16N2OS
纯度 : 98%
分子量 : 332.42
MDL号 : MFCD01005305
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(54.15 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
生物活性
靶点

  • JNK2

    JNK2, pIC50:6.5

  • JNK3

    JNK3, pIC50:6.7
描述 c-Jun N-terminal kinase (JNK) is implicated in various human diseases, including cancer, inflammatory disorders, and neurodegeneration. JNK inhibitor IX is a potent JNK inhibitor with pIC50 values of 6.5 and 6.7 for JNK2 and JNK3, respectively[3]. Pre-treatment of human dermal fibroblasts with JNK inhibitor IX (10μM) 30min before chromium exposure significantly reduces caspase-3 activity compared to the group only treated with chromium[4]. Treatment of myeloid cells with JNK inhibitor IX (10μM) for 24 h significantly reduced JNK phosphorylation and increased apoptotic cell death in response to imatinib mesylate[5].
作用机制 JNK inhibitor IX is a potent, ATP-competitive inhibitor of both JNK2 and JNK3[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.04mL

3.01mL

1.50mL

30.08mL

6.02mL

3.01mL
参考文献

[1]Rudolf E, Cervinka M. Trivalent chromium activates Rac-1 and Src and induces switch in the cell death mode in human dermal fibroblasts. Toxicol Lett. 2009 Aug 10;188(3):236-42.

[2]Angell RM, Atkinson FL, et al. N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1296-301.

[3]Angell RM, Atkinson FL, Brown MJ, et al. N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. Bioorg Med Chem Lett. 2007;17(5):1296-1301. doi:10.1016/j.bmcl.2006.12.003

[4]Rudolf E, Cervinka M. Trivalent chromium activates Rac-1 and Src and induces switch in the cell death mode in human dermal fibroblasts. Toxicol Lett. 2009;188(3):236-242. doi:10.1016/j.toxlet.2009.04.019

[5]Mancini M, Veljkovic N, Corradi V, et al. 14-3-3 ligand prevents nuclear import of c-ABL protein in chronic myeloid leukemia. Traffic. 2009;10(6):637-647. doi:10.1111/j.1600-0854.2009.00897.x