Lavendustin B |
| カタログ番号GC45494 |
ラベンダスチン B は、HIV-1 インテグラーゼと LEDGF/p75 との相互作用の阻害剤であり、IC50 は 94.07 μM です。 Lavendustin B は、Ki が 15 μM の ATP 競合 GLUT1 阻害剤です。 Lavendustin B は、チロシンキナーゼの弱い阻害剤でもあります。
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Cas No.: 125697-91-8
Sample solution is provided at 25 µL, 10mM.
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Lavendustin B is a competitive inhibitor of glucose transporter 1 (Glut1; Ki = 15 μM).1 It is also an inhibitor of the interaction between HIV-1 integrase and LEDGF/p75 (IC50 = 94.07 μM).2 Lavendustin B is a weak inhibitor of tyrosine kinases (IC50 = 0.49 μg/ml) and has been used as a negative control for the protein tyrosine kinase inhibitor lavendustin A .3,4,5
References
1. Vera, J.C., Reyes, A.M., VelÁsquez, F.V., et al. Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. Biochemistry 40(3), 777-790 (2001).
2. De Luca, L., Morreale, F., Christ, F., et al. New scaffolds of natural origin as Integrase-LEDGF/p75 interaction inhibitors: Virtual screening and activity assays. Eur. J. Med. Chem. 68, 405-411 (2013).
3. Onoda, T., Iinuma, H., Sasaki, Y., et al. Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J. Nat. Prod. 52(6), 1252-1257 (1989).
4. Hu, D.E., and Fan, T.-P.D. Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A. Br. J. Pharmacol. 114(2), 262-268 (1995).
5. Alioua, A., Mahajan, A., Nishimaru, K., et al. Coupling of c-Src to large conductance voltage- and Ca2+-activated K+ channels as a new mechanism of agonist-induced vasoconstriction. Proc. Natl. Acad. Sci. USA 99(22), 14560-14565 (2002).
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