MedChemExpress - Model N3PT -13860-66-7

N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an Kd value of 22 nM (Apo-TK, transketolase lacking bound thiamine)[1].

N3PT

MCE China：N3PT

Brand：MedChemExpress (MCE)

Cat. No.HY-16339

CAS：13860-66-7

Synonyms：N3-pyridyl thiamine

Purity：99.56%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：N3PT (N3-pyridyl thiamine) is a potent and selective transketolase inhibitor. N3PT is pyrophosphorylated and then binds to transketolase with an Kd value of 22 nM (Apo-TK, transketolase lacking bound thiamine).

In Vitro：Arginase inhibitor 1inhibits human arginases I and II with IC50s of 223±22.3 and 509±85.1 nM, respectively, and is active in a recombinant cellular assay overexpressing human arginase I (CHO cells). Arginase inhibitor 1 is a novel second generation arginase inhibitor with significant activity in a rat model of myocardial ischemia/reperfusion injury (MI/RI). Arginase inhibitor 1 is potent against hARG I in both in vitro enzyme and cellular assays. The IC50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI[1].

In Vivo：N3PT (compound 1) (100 mg/kg; i.v.; twice a day; 2 weeks) shows inhibitory effect on transketolase activity without significantly anti-tumor activity in HCT-116 tumor-bearing nude mice[1].

IC50 & Target：transketolase[1] In Vitro Arginase inhibitor 1inhibits human arginases I and II with IC50s of 223±22.3 and 509±85.1 nM, respectively, and is active in a recombinant cellular assay overexpressing human arginase I (CHO cells). Arginase inhibitor 1 is a novel second generation arginase inhibitor with significant activity in a rat model of myocardial ischemia/reperfusion injury (MI/RI). Arginase inhibitor 1 is potent against hARG I in both in vitro enzyme and cellular assays. The IC50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> N3PT Related Antibodies

References：

[1]. Thomas AA, et al. Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. [Content Brief]

[2]. Jeno Gyuris, May Han, Ronan C, N3-pyridyl-thiamine and its use in cancer treatments. Patent Numeber: WO2005094803 A2

[3]. Allen A. Thomas, Josh Ballard, Bryan Bernat. Potent and Selective Thiamine Antagonists That Inhibit Transketolase.

[4]. 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. [Content Brief]

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MedChemExpress - Model N3PT -13860-66-7

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N3PT