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BIO-acetoxime

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Chemical Structure| 667463-85-6 同义名 : BIA;GSK-3 Inhibitor X;(2′Z,3′E)-6-Bromoindirubin-3′-acetoxime, 6-Bromoindirubin acetoxime, 6-Bromoindirubin-3′-acetoxime, BIA
CAS号 : 667463-85-6
货号 : A731227
分子式 : C18H12BrN3O3
纯度 : 95%
分子量 : 398.21
MDL号 : MFCD09037533
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 20 mg/mL(50.22 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
靶点
  • GSK-3α

    GSK-3α, IC50:10 nM

  • GSK-3β

    GSK-3β, IC50:10 nM

描述 In mammals, different genes encode two closely related glycogen synthase kinase-3 (GSK-3) enzymes, GSK-3α and GSK-3β which function in Wnt signal-transducing pathways, insulin action, apoptosis and circadian rhythm. BIO-acetoxime is a potent and selective GSK-3 inhibitor, with IC50s of 10 nM for both GSK-3α and GSK-3β. It also shows weak effect on CDK5/p35, CDK2/cyclin A, and CDK1/cyclin B with IC50s of 2.4, 4.3 and 63 μM, respectively[3]. Treatment of OC3 cells with BIO-acetoxime (5 or 10 μM) prevented HSV-1-induced cell death. In addition, BIO-acetoxime alleviated HSV-1-induced apoptosis. In oral epithelial cells, BIO-acetoxime inhibited HSV-1 propagation in a dose-dependent manner[4]. In a rat limbic seizure model, the pilocarpine-induced seizures are indeed significantly attenuated after i.p. injection of 0.5 mg/kg BIO-acetoxime[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.56mL

2.51mL

1.26mL

25.11mL

5.02mL

2.51mL

参考文献

[1]Hsu MJ, Hung SL. Antiherpetic potential of 6-bromoindirubin-3'-acetoxime(BIO-acetoxime) in human oral epithelial cells. Arch Virol. 2013 Jun;158(6):1287-96.

[2]Polychronopoulos P, Magiatis P, et al. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem. 2004 Feb 12;47(4):935-46.

[3]Meijer L, Skaltsounis AL, et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66

[4]Hsu MJ, Hung SL. Antiherpetic potential of 6-bromoindirubin-3'-acetoxime (BIO-acetoxime) in human oral epithelial cells. Arch Virol. 2013 Jun;158(6):1287-96

[5]Aourz N, Serruys AK, et al. Identification of GSK-3 as a Potential Therapeutic Entry Point for Epilepsy. ACS Chem Neurosci. 2019 Apr 17;10(4):1992-2003