AS601245

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Chemical Structure| 345987-15-7 同义名 : JNK Inhibitor V;c-Jun N-terminal Kinase Inhibitor V
CAS号 : 345987-15-7
货号 : A163603
分子式 : C20H16N6S
纯度 : 98%
分子量 : 372.446
MDL号 : MFCD07772196
存储条件：

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

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

DMSO: 9 mg/mL(24.16 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
描述 c-Jun N-terminal kinases (JNK) are a family of mitogen-activated protein kinases that can be activated in response to inflammatory cytokines, ischemia, UV irradiation, and heat shock. AS-601245 is a benzothiazole acetonitrile derivative that inhibits three human JNK isoforms JNK1, JNK2, and JNK3 with IC50 values of 150, 220, and 70 nM, respectively. It also exhibited 10- to 20-fold selectivity over c-Raf, CDK2, and c-src and > 50- to 100-fold selectivity over Ser/Thr- and Tyr-protein kinases. The oral administration of C3H/HEN mice with AS-601245 at 0.3, 1, 3, and 10 mg/kg decreased LPS-induced TNF-α release in a dose-dependent manner. The i.p. injection of AS601245 (40, 60, and 80 mg/kg) 1 h before and 24 h after the reperfusion dose-dependently decreased hippocampal damage in mice (16, 74, and 83%, respectively). When mice were injected with AS-601245 15 min and 24 h after the reperfusion at the above-mentioned doses, the hippocampal damage was decreased by 29, 40, and 52%, respectively. The i.p. administration of AS-601245 at 60 mg/kg led to a significant reduction in the number of phospho-c-Jun-stained neurons. AS-601245 at the doses of 18 and 60 mg/kg significantly reduced the size of cortical lesions in mice following middle cerebral artery occlusion by 27 and 52%, respectively[2].
作用机制 AS-601245 is a structurally unique JNK inhibitor. It inhibits isolated human JNK3 in an ATP-competitive manner[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.42mL

2.68mL

1.34mL

26.85mL

5.37mL

2.68mL
参考文献

[1]Carboni S, Boschert U, et al. AS601245, a c-Jun NH2-terminal kinase (JNK) inhibitor, reduces axon/dendrite damage and cognitive deficits after global cerebral ischaemia in gerbils. Br J Pharmacol. 2008 Jan;153(1):157-63.

[2] Carboni S, Hiver A, Szyndralewiez C, Gaillard P, Gotteland JP, Vitte PA. AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. J Pharmacol Exp Ther. 2004;310(1):25‐32. doi:10.1124/jpet.103.064246