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CAS No.: 4452-06-6

ZM 449829 Catalog No. CSN23211

Synonyms: JAK3 Inhibitor V;Janus-Associated Kinase 3 Inhibitor V

Potent, selective JAK3 inhibitor

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述The JAK/ATAT signaling pathway involves two protein families, the JAKs and the STATs. The JAK/STAT pathway forms a critical node affecting multiple signaling pathways in both the innate and adaptive immune responses. Janus kinase 2 (JAK2) belongs to the non-receptor tyrosine kinase family. Upon tyrosine receptor phosphorylation, JAKs are activated and, in turn, phosphorylate the tyrosine motifs in the cytoplasmic tail of the receptor, which allows for STAT binding . The JAK protein family consists of four members [JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2)], whereas the STAT family consists of seven members (STAT1, STAT2, STAT3, STAT4, STAT5A, STAT5B, and STAT6). ZM39923 is a Janus kinase inhibitor with pIC₅₀ values of 6.8 nM, 5.0 nM, 4.7 nM, and < 5.0 nM for JAK3, EGFR, JAK1 and CDK4 respectively, it can also inhibit human tissue transglutaminase (TGM2) with IC₅₀ of 10 nM^[1]. In a vivo study, rats were treated with vehicle, morphine (300 mg/kg), the delta-opioid agonist fentanyl isothiocynate (FIT, 10 mg/kg), or the GSK inhibitor SB-216763 (SB21, 600 mg/kg) 10 min before ischemia. Five minutes before opioid or SB21 treatment, some rats received JAK3 inhibitor ZM-449829 (3 mg/kg). ZM-449829, a more selective inhibitor for JAK3 that also inhibits the EGF receptor was shown not to affect opioid-induced cardioprotection. In a dialysis experiment, it was indicated that chemicals targeted Ca⁺² - TGM2. In the absence of Ca⁺², there was only 20%- 40% inhibition by ZM39923, vitamin K3, vitamin K2, and Me-3,4-dephostatin, whereas >90% inhibition was observed by ZM449829^[1].
作用机制ZM 449829 binds competitively to the JAK3 ATP-binding site.
参考文献

[1] Lai TS, Liu Y, Tucker T, Daniel KR, Sane DC, Toone E, Burke JR, Strittmatter WJ, Greenberg CS. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008 Sep 22;15(9):969-78. doi: 10.1016/j.chembiol.2008.07.015. PMID: 18804034; PMCID: PMC2637080.

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
- 5.4879 mL
- 27.4397 mL
- 54.8794 mL
- 5 mM
- 1.0976 mL
- 5.4879 mL
- 10.9759 mL
- 10 mM
- 0.5488 mL
- 2.7440 mL
- 5.4879 mL

技术信息

CAS号

4452-06-6

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

C13H10O

运输

蓝冰

分子量

182.22

别名

JAK3 Inhibitor V;Janus-Associated Kinase 3 Inhibitor V

溶解度

DMSO	200.0 mg/mL (1097.6 mM)
Water	insoluble

动物实验配方

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