IDO-IN-2 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IC50 = 0.097 ?M 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
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) inhibitorsBioorg. 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 modelsInt. J. Immunopathol. Pharmacol.322058738418787991(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 amygdalaBiochem. Pharmacol.177113926(2020)