N3PT

Transketolase(TK) inhibitor CAS# 13860-66-7

N3PT

Catalog No. BCC1782----Order now to get a substantial discount!

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Chemical structure

N3PT

3D structure

Chemical Properties of N3PT

Cas No. 13860-66-7 SDF Download SDF
PubChem ID 66970987 Appearance Powder
Formula C13H19Cl2N3OS M.Wt 336.28
Type of Compound N/A Storage Desiccate at -20°C
Synonyms N3-pyridyl thiamine
Solubility DMSO : 2.86 mg/mL (8.50 mM; Need ultrasonic)
Chemical Name 2-[3-[(2-amino-6-methylpyridin-3-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol;chloride;hydrochloride
SMILES CC1=NC(=C(C=C1)C[N+]2=CSC(=C2C)CCO)N.Cl.[Cl-]
Standard InChIKey ZLGKCAQWOASSTP-UHFFFAOYSA-M
Standard InChI InChI=1S/C13H18N3OS.2ClH/c1-9-3-4-11(13(14)15-9)7-16-8-18-12(5-6-17)10(16)2;;/h3-4,8,17H,5-7H2,1-2H3,(H2,14,15);2*1H/q+1;;/p-1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of N3PT

DescriptionN3PT(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: transketolase in 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].

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.

N3PT Dilution Calculator

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N3PT Molarity Calculator

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Preparing Stock Solutions of N3PT

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9737 mL 14.8686 mL 29.7371 mL 59.4742 mL 74.3428 mL
5 mM 0.5947 mL 2.9737 mL 5.9474 mL 11.8948 mL 14.8686 mL
10 mM 0.2974 mL 1.4869 mL 2.9737 mL 5.9474 mL 7.4343 mL
50 mM 0.0595 mL 0.2974 mL 0.5947 mL 1.1895 mL 1.4869 mL
100 mM 0.0297 mL 0.1487 mL 0.2974 mL 0.5947 mL 0.7434 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on N3PT

Description: IC50 Value: 22 nM(Apo-TK) ; 26 nM (EC50, Cellular TK) [1] N3PT is a potent and selective TK inhibitor both in vitro and in vivo. in 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]. Clinical trial: N/A

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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.

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