N3PT

Modify Date: 2024-01-04 23:22:21

N3PT Structure
N3PT structure
Common Name N3PT
CAS Number 13860-66-7 Molecular Weight 336.28000
Density N/A Boiling Point N/A
Molecular Formula C13H19Cl2N3OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of N3PT


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].

 Names

Name 3-[(2-Amino-6-methyl-3-pyridinyl)methyl]-5-(2-hydroxyethyl)-4-met hyl-1,3-thiazol-3-ium chloride hydrochloride (1:1:1)
Synonym More Synonyms

 N3PT Biological Activity

Description 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].
Related Catalog
References

[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.

 Chemical & Physical Properties

Molecular Formula C13H19Cl2N3OS
Molecular Weight 336.28000
Exact Mass 335.06300
PSA 91.26000
Storage condition 2-8℃

 Synthetic Route

~%

N3PT Structure

N3PT

CAS#:13860-66-7

Literature: Matsukawa; Matsuno Yakugaku Zasshi, 1944 , vol. 64, # 3 p. 145,150 Chem.Abstr., 1951 , p. 4724

~%

N3PT Structure

N3PT

CAS#:13860-66-7

Literature: Dornow; Hargesheimer Chemische Berichte, 1953 , vol. 86, p. 461,464

~%

N3PT Structure

N3PT

CAS#:13860-66-7

Literature: Dornow; Hargesheimer Chemische Berichte, 1953 , vol. 86, p. 461,464

 Synonyms

3-(2-amino-6-methyl-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazolium,chloride hydrochloride
2-(2H-pyrazol-3-yl)-5-(trifluoromethyl)aniline
3-(2-Amino-6-methyl-[3]pyridylmethyl)-5-(2-hydroxy-aethyl)-4-methyl-thiazolium,Chlorid-hydrochlorid
3-(2-amino-6-methyl-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride
2-(1(2)H-pyrazol-3-yl)-5-trifluoromethyl-aniline
3-(2-Amino-4-trifluormethylphenyl)pyrazol
3-(2-amino-6-methyl-[3]pyridylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazolium,chloride-hydrochloride
N3PT