Vidofludimus (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 value of 134nmol/L for human DHODH [1].
Vidofludimus (4SC-101, SC12267) has been reported to dose-dependently inhibit DHODH in an in vitro enzyme assay with IC50 values of 0.134μmol/L, 1.29μmol/L, 10.6μmol/L and 12.9μmol/L in human DHODH, rat DHODH, mouse DHODH and human PBMC, respectively [1]. In addition, Vidofludimus has shown the inhibition of proliferation in phytohemagglutinin-induced lymphocytes with an IC50 value of ~13μmol/L. Moreover, Vidofludimus has been revealed to concentration-dependently inhibit phytohemagglutinin-stimulated interukin-17 secretion from human peripgeral blppd mononuclear cell lines (PBMCs) with an IC50 value of 6 μmol/L [2].
References:
[1] Kulkarni OP1, Sayyed SG, Kantner C, Ryu M, Schnurr M, Sárdy M, Leban J, Jankowsky R, Ammendola A, Doblhofer R, Anders HJ. 4SC-101, a novel small molecule dihydroorotate dehydrogenase inhibitor, suppresses systemic lupus erythematosus in MRL-(Fas) lpr mice. Am J Pathol. 2010 Jun;176(6):2840-7.
[2] Fitzpatrick LR1, Deml L, Hofmann C, Small JS, Groeppel M, Hamm S, Lemstra S, Leban J, Ammendola A. 4SC-101, a novel immunosuppressive drug, inhibits IL-17 and attenuates colitis in two murine models of inflammatory bowel disease. Inflamm Bowel Dis. 2010 Oct;16(10):1763-77.