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SPRi 3

Names

[ CAS No. ]:
1292285-54-1

[ Name ]:
SPRi 3

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Others >> Others

[Target]

IC50: 74 nM (sepiapterin reductase)[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H18N2O3

[ Molecular Weight ]:
262.30

Related Compounds