ZM39923 HCl

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Chemical Structure| 1021868-92-7 同义名 : ZM 39923 (hydrochloride);Janus-Associated Kinase 3 Inhibitor IV;JAK3 Inhibitor IV;ZM39923 hydrochloride
CAS号 : 1021868-92-7
货号 : A107403
分子式 : C23H26ClNO
纯度 : 97%
分子量 : 367.912
MDL号 : MFCD04974534
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: 45 mg/mL(122.31 mM)，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

H2O: 1 mg/mL(2.72 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • JAK1

    JAK1, pIC50:4.4

  • JAK3

    JAK3, pIC50:7.1
描述 Janus kinase 3 (JAK3) is a tyrosine kinase mainly expressed in lymphoid cells. ZM39923 hydrochloride is a potent JAK3 inhibitor with a pIC50 value of 7.1±0.3. However, it is a weak inhibitor for EGF-R and Janus kinase 1 with pIC50 values of 5.6 and 4.4, respectively. ZM39923 hydrochloride showed insignificant inhibitory effect against tyrosine kinases Lck and CDK4 with a pIC50 of less than 5.0.[3] ZM39923 hydrochloride is also a potent inhibitor of tissue transglutaminase with an IC50 of 10nM.[4] The CCL19-induced phosphorylation of JAK3 in PCI-37B cells was inhibited by 10µM ZM39923 compared with the group treated with CCL19 alone. In SCCHN cells, ZM39923 at 10µM significantly blocked CCL19-induced wound closure rate compared with the control group.[5]
作用机制 ZM39923 hydrochloride is a potent inhibitor for both JAK3 and tissue transglutaminase.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.59mL

2.72mL

1.36mL

27.18mL

5.44mL

2.72mL
参考文献

[1]Fraering PC, Ye W, et al. gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site. J Biol Chem. 2005 Dec 23;280(51):41987-96.

[2]Brown GR, Bamford AM, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9.

[3]Brown GR, Bamford AM, Bowyer J, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000;10(6):575-579. doi:10.1016/s0960-894x(00)00051-2

[4]Lai TS, Liu Y, Tucker T, et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008;15(9):969-978. doi:10.1016/j.chembiol.2008.07.015

[5]Zhang Z, Liu F, Li Z, Wang D, Li R, Sun C. Jak3 is involved in CCR7-dependent migration and invasion in metastatic squamous cell carcinoma of the head and neck. Oncol Lett. 2017;13(5):3191-3197. doi:10.3892/ol.2017.5861