N3PT |
Catalog No.GC36677 |
N3PT (N3-피리딜 티아민)는 강력하고 선택적인 트랜스케톨라아제 억제제입니다. N3PT는 이화학적으로 인산화되어 Kd 값이 22 nM (결합된 티아민이 없는 Apo-TK, 트랜스케톨라아제)로 transketolase에 결합됩니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13860-66-7
Sample solution is provided at 25 µL, 10mM.
N3PT(N3-pyridyl thiamine) is a potent and selective transketolase(TK) inhibitor (IC50= 22 nM for Apo-TK) both in vitro and in vivo.IC50 Value: 22 nM( Apo-TK) ; 26 nM (EC50, Cellular TK) [1]Target: transketolasein vitro: N3PT inhibits transketolase activity in a cell based assay. Competitive inhibition of TK by N3PT in cells treated with increasing doses of thiamine, expressed as percentage enzymatic activity (the slope of initial linear range) of controls not treated with compounds [1].in vivo: Tumors were induced in mice at day 0 and mice were then treated at day 7 with vehicle alone or with N3PT [2]. Low-thiamine diet enhances the sensitivity to N3PT inhibition of TK in spleen. Animals were switched to diets containing 16.5 mg/kg (unchanged), 5 mg/kg, 1 mg/kg, or 0 mg/kg thiamine, from a normal chow containing 16.5mg/kg thiamine [1].
[1]. Allen A. Thomas, Josh Ballard, Bryan Bernat. Potent and Selective Thiamine Antagonists That Inhibit Transketolase. [2]. Jeno Gyuris, May Han, Ronan C, N3-pyridyl-thiamine and its use in cancer treatments. Patent Numeber: WO2005094803 A2 [3]. Thomas AA, De Meese J, Le Huerou Y, Non-charged thiamine analogs as inhibitors of enzyme transketolase. Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12.
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