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CAS No.: 345987-15-7

AS601245 Catalog No. CSN18229

Synonyms: JNK Inhibitor V;c-Jun N-terminal Kinase Inhibitor V

AS-601245 is an inhibitor of the c-Jun NH2-terminal kinase (JNK) (hJNK1: IC50=150nM, hJNK2: IC50=220nM and hJNK3: IC50=70 nM), has neuroprotective properties.

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6850 mL
- 13.4248 mL
- 26.8495 mL
- 5 mM
- 0.5370 mL
- 2.6850 mL
- 5.3699 mL
- 10 mM
- 0.2685 mL
- 1.3425 mL
- 2.6850 mL

技术信息

CAS号

345987-15-7

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H16N6S

运输

蓝冰

分子量

372.45

别名

JNK Inhibitor V;c-Jun N-terminal Kinase Inhibitor V

溶解度

DMSO	10.0 mg/mL (26.8 mM) warming

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