Lavendustin B

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Chemical Structure| 125697-91-8 同义名 : -
CAS号 : 125697-91-8
货号 : A597168
分子式 : C21H19NO5
纯度 : 99%
分子量 : 365.38
MDL号 : MFCD00133446
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

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

DMSO: 50 mg/mL(136.84 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
生物活性
描述 HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells[2]. HIV-1 IN acts as a key component of the Retroviral Pre-Integration Complex (PIC)[3].the HIV-1 replication depends not only on distinct steps but also lens epithelium-derived growth factor/p75 (LEDGF/p75)[4]. HIV-1 integrase (IN) inhibitors are primary drugs in Highly active antiretroviral therapy (HAART) regimens targeting integration step in the HIV-1 life cycle[5]. Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases[6]. In HL-60 cells, Lavendustin B (0-1000 µM) inhibits the uptake of methylglucose, deoxyglucose, and dehydroascorbic acid in human erythrocytes in a dose-dependent manner, with 50% inhibition observed at approximately 10-30 µM. Moreover, increasing concentrations of Lavendustin B inhibited, in a dose-dependent manner, the binding of cytochalasin B to human erythrocyte membranes[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.68mL

2.74mL

1.37mL

27.37mL

5.47mL

2.74mL
参考文献

[1]Vera JC, Reyes AM, Velásquez FV, Rivas CI, Zhang RH, Strobel P, Slebe JC, Núñez-Alarcón J, Golde DW. Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. Biochemistry. 2001 Jan 23;40(3):777-90. doi: 10.1021/bi001660j. PMID: 11170395.

[2] Maninder Kaur,et al. Structure Based Drug Design: Clinically Relevant HIV-1 Integrase Inhibitors.

[3] Jae-Hyun Park,et al. Non-Cryogenic Structure and Dynamics of HIV-1 Integrase Catalytic Core Domain by X-ray Free-Electron Lasers. Int J Mol Sci. 2019 Apr 20;20(8):1943.

[4] Yang Li,et al. Targeting HIV-1 integrase with strand transfer inhibitors. Drug Discov Today. 2015 Apr;20(4):435-49.

[5] Xiqiang Cheng,et al. Identification of spirocyclic or phosphate substituted quinolizine derivatives as novel HIV-1 integrase inhibitors: a patent evaluation of WO2016094197A1, WO2016094198A1 and WO2016154527A1. Expert Opin Ther Pat. 2017 Nov;27(11):1277-1286.

[6]Fatima E Agharbaoui, et al. Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase. Eur J Med Chem. 2016 Nov 10;123:673-683.

[7]J C Vera, et al. Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. Biochemistry. 2001 Jan 23;40(3):777-90.