OSMI-4 |
رقم الكتالوجGC31517 |
OSMI-4 هو أفضل مثبط OGT تم الإبلاغ عنه حتى الآن والشكل النشط لـ OSMI-4 له تأثير تثبيطي بتركيز منخفض النانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2260791-14-6
Sample solution is provided at 25 µL, 10mM.
OSMI-4 is the best OGT inhibitor reported to date and the active form of OSMI-4 has low nanomolar binding affinity [1]. OSMI-4 has a chlorine substituent on the quinolinone ortho to the sulfonamide, thus allowing the molecule to bind tighter in the uridine binding pocket within the enzyme’s active site [2]. The free acid and ester forms of OSMI-4 are OSMI-4a and OSMI-4b, respectively.
OSMI-4 has further enhanced binding affinities to the enzyme with a Kd of 8 nM. The IC50 of OSMI-4a and OMSI-4b are 1.5 and 0.5μM, respectively [3]. The EC50 of OSMI-4 in HEK293T cells is 3 μM [1].
References:
[1].Martin SES, Tan ZW, Itkonen HM, Duveau DY, Paulo JA, Janetzko J, Boutz PL, Törk L, Moss FA, Thomas CJ, Gygi SP, Lazarus MB, Walker S. Structure-Based Evolution of Low Nanomolar O-GlcNAc Transferase Inhibitors. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545.
[2].Ju Kim E. O-GlcNAc Transferase: Structural Characteristics, Catalytic Mechanism and Small-Molecule Inhibitors. Chembiochem. 2020 Nov 2;21(21):3026-3035.
[3].Loi EM, Weiss M, Pajk S, Gobec M, Tomašič T, Pieters RJ, Anderluh M. Intracellular Hydrolysis of Small-Molecule O-Linked N-Acetylglucosamine Transferase Inhibitors Differs among Cells and Is Not Required for Its Inhibition. Molecules. 2020 Jul 25;25(15):3381.
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