Bioactivity | PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the Ki values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively. PSB-06126 acts on human NTPDase 3 with an IC50 value of 7.76 μM and a Ki value of 4.39 μM[1][2]. | |||||||||
Target | Ki: 0.33 μM (rat NTPDase 1), 19.1 μM (rat NTPDase 2), 2.22 μM (rat NTPDase 3),4.39 μM (human NTPDase 3). | |||||||||
Invitro | PSB 06126 (3 μM) blocks NTPDase3 overexpressed in mesenchymal stem cells (MSCs), leading to increased extracellular ATP levels and osteogenic differentiation and mineralisation of MSCs through activation of P2X7 and P2Y6 receptors[3]. | |||||||||
Name | PSB-06126 | |||||||||
CAS | 1052089-16-3 | |||||||||
Formula | C24H15N2NaO5S | |||||||||
Molar Mass | 466.44 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Younis Baqi, et al. Ecto-nucleotidase inhibitors: recent developments in drug discovery. Mini Rev Med Chem. 2015;15(1):21-33. [2]. Amelie Fiene, et al. Fluorescence polarization immunoassays for monitoring nucleoside triphosphate diphosphohydrolase (NTPDase) activity. Analyst. 2015 Jan 7;140(1):140-8. [3]. J B Noronha-Matos, et al. Mesenchymal Stem Cells Ageing: Targeting the "Purinome" to Promote Osteogenic Differentiation and Bone Repair. J Cell Physiol. 2016 Sep;231(9):1852-61. |