POM 1

Biological Activity

POM 1 is an inhibitor of Ecto-NTPDases that displays minor selectivity for NTPDases 1 and 2 over NTPDase 3 and P2Y₁₂ (K_i values are 2.58, 3.26, > 10 and 28.8 μM for NTPDase 1, NTPDase 3, P2Y₁₂ and NTPDase 2 respectively). Abolishes renal protection induced by ischemic preconditioning. Inhibits synaptic transmission at hippocampal CA1 pyramidal synapses and at the cerebellar parallel fiber-Purkinje cell (PF) synapse.

Technical Data

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.

Background References

1. Adoptive transfer of human gingiva-derived mesenchymal stem cells ameliorates collagen-induced arthritis via suppression of Th1 and Th17 cells and enhancement of regulatory T cell differentiation.
   Chen M, Su W, Lin X, Guo Z, Wang J, Zhang Q, Brand D, Ryffel B, Huang J, Liu Z, He X, Le A, Zheng S
   Arthritis Rheum, 2013;65(5):1181-93.
2. Increased CD39 Nucleotidase Activity on Microparticles from Patients with Idiopathic Pulmonary Arterial Hypertension.
   Visovatti SH, Hyman MC, Bouis D
   PLoS ONE, 2012;7(7):e40829.
3. A negative feedback loop mediated by STAT3 limits human Th17 responses.
   Purvis H, Anderson A, Young D, Isaacs J, Hilkens C
   J Immunol, 2015;193(3):1142-50.
4. Hypoxia inducible factor HIF-1 promotes myeloid-derived suppressor cells accumulation through ENTPD2/CD39L1 in hepatocellular carcinoma
   DK Chiu, AP Tse, IM Xu, J Di Cui, RK Lai, LL Li, HY Koh, FH Tsang, LL Wei, CM Wong, IO Ng, CC Wong
   Nat Commun, 2017;8(1):517.
5. Polyoxometalates - a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors.
   Muller et al.
   Bioorg.Med.Chem.Lett., 2006;16:5943
6. Contribution of E-NTPDase1 (CD39) to renal protection from ischemia-reperfusion injury.
   Grenz et al.
   FASEB J., 2007;21:2863

Product Datasheets