IDO-IN-2

IDO-IN-2 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IC₅₀ = 0.097 µM in HeLa cells).¹ In vivo, IDO-IN-2 (100 mg/kg) decreases intratumor levels of Ki67, a marker of cell proliferation, and reduces tumor weight in a GL261 murine glioma heterotopic transplantation model.² It also decreases mechanical and thermal hypersensitivity, improves novel object recognition, and decreases anterior cingulate cortex (ACC) and amygdala levels of IDO1 in a rat model of neuropathic pain induced by spinal nerve ligation (SNL).³

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1. Williams, D.K., Markwalder, J.A., Balog, A.J., et al. Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. Bioorg. Med. Chem. Lett. 28(4), 732-736 (2018).

2. Sun, S., Du, G., Xue, J., et al. PCC0208009 enhances the anti-tumor effects of temozolomide through direct inhibition and transcriptional regulation of indoleamine 2,3-dioxygenase in glioma models. Int. J. Immunopathol. Pharmacol. 32, 2058738418787991 (2018).

3. Wang, Y., Li, C.-M., Han, R., et al. PCC0208009, an indirect IDO1 inhibitor, alleviates neuropathic pain and co-morbidities by regulating synaptic plasticity of ACC and amygdala. Biochem. Pharmacol. 177, 113926 (2020).