Bioactivity | SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels[1][2][3]. |
Target | IC50: 74 nM (sepiapterin reductase) |
Invitro | SPR inhibitor 3 (SPRi3) also significantly reduces SPR activity in mouse primary cultures of sensory neurons (IC50=0.45 μM) without affecting the activity of GTP cyclohydroxylase 1 enzyme (GCH1)[1]. |
Name | SPR inhibitor 3 |
CAS | 1292285-54-1 |
Formula | C14H18N2O3 |
Molar Mass | 262.30 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Reference | [1]. Latremoliere A, et al. Reduction of Neuropathic and Inflammatory Pain through Inhibition of the Tetrahydrobiopterin Pathway. Neuron. 2015 Jun 17;86(6):1393-406. [2]. Cronin SJF, et al. The metabolite BH4 controls T cell proliferation in autoimmunity and cancer. Nature. 2018 Nov;563(7732):564-568. [3]. Haruki H, et al. Tetrahydrobiopterin Biosynthesis as a Potential Target of the Kynurenine Pathway Metabolite Xanthurenic Acid. J Biol Chem. 2016 Jan 8;291(2):652-7. |