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Description: Potent and selective O-GlcNAcase (OGA) inhibitor
Chemical Name: N-[(1-Methyl-1H-imidazol-4-yl)methyl]-4-(4-methyl-1-piperidinyl)-2-pyrimidinamine
Purity: ≥98% (HPLC)

Biological Activity for TP-040

TP-040 is a potent and selective O-GlcNAcase (OGA) inhibitor (IC50 = 46 nM). It increases the level of O-GlcNAcylated protein in human neuroblastoma SH-SY5Y cells (EC50 = 450 nM). It is suitable for in vivo studies and exhibits brain permeability.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TP-040 probe summary on the SGC website.

Technical Data for TP-040

M. Wt 286.38
Formula C15H22N6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2757254-99-0
PubChem ID 162640825
Smiles CN1C=NC(CNC2=NC=CC(N3CCC(CC3)C)=N2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TP-040

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 28.64 100
DMSO 28.64 100

Preparing Stock Solutions for TP-040

The following data is based on the product molecular weight 286.38. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.49 mL 17.46 mL 34.92 mL
5 mM 0.7 mL 3.49 mL 6.98 mL
10 mM 0.35 mL 1.75 mL 3.49 mL
50 mM 0.07 mL 0.35 mL 0.7 mL

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References for TP-040

References are publications that support the biological activity of the product.

Tawada et al (2021) Discovery of a novel and brain-penetrant O-GlcNAcase inhibitor via virtual screening, structure-based analysis, and rational lead optimization. J.Med.Chem. 64 1103 PMID: 33404239

If you know of a relevant reference for TP-040, please let us know.

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Citations for TP-040

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