125697-91-8

125697-91-8 structure

Name: lavendustin B
Chemical Name: Lavendustin B
CAS Number: 125697-91-8
Molecular Formula: C₂₁H₁₉NO₅
Molecular Weight: 365.37900
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIV Integrase
Create Date: 2018-04-05 08:00:00
Modify Date: 2024-01-11 13:50:52
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[1][2].

Name	Lavendustin B
Synonyms	5-[bis[(2-hydroxyphenyl)methyl]amino]-2-hydroxybenzoic acid

Description	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[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Tyrosinase Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase
Target	GLUT1:15 μM (Ki) HIV-1 integrase interaction with LEDGF/p75:94.07 μM (IC50)
In Vitro	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[1].
References	[1]. J C Vera, et al. Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. Biochemistry. 2001 Jan 23;40(3):777-90. [2]. 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.