NLG919 is an orally available potent inhibitor of the indoleamine-2,3- dioxygenase (IDO) pathway, a crucial pathway involved in allergic inflammation that mediates immunosuppressive effects through metabolization of tryptophan to kynurenine. NLG919 affects differentiation and proliferation of T cells by inducing downstream signaling via GCN2, mTOR and AHR, with values of Ki = 7 nM and EC50 = 75 nM. NLG919 is being investigated for the treatment of immunosuppression associated with cancer.

1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol, IDO inhibitor

≥98%

NLG919 potently blocks IDO-induced T cell suppression and restored T cell responses with a reported ED50 of 80 nM in vitro. NLG919 reduced the concentration of plasma and tissue kynurenine by ~50% after a single dose in mice. NLG919 enhanced the antitumor responses of naïve, resting pmel-1 T-cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA in mice bearing B16F10 tumors.

Soluble in DMSO at 15 mg/ml.

White powder

Store as supplied at or below -20°C for up to 3 years. Stable in DMSO at -80°C for up to 6 months.

1. Driessens, G., et al., J. Immunother. Cancer. 2014; 2(Suppl 3):195.
2. Nayak, A., et al. J. Immunother. Cancer. 2014; 2(Suppl 3): 250.

Immunotherapy

Inhibitors/Activators