Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
eIF4E-IN-1 (WO2021003194A1, compound Y), is a highly effective inhibitor of eIF4E, a key protein involved in immunosuppression. By targeting immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO, eIF4E-IN-1 functions to disrupt immune suppression and promote immune release in specific diseases such as cancer and infectious diseases.
(Rac)-Indoximod (1-Methyl-DL-tryptophan) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO). Combined treatment with IFN-γ and (Rac)-Indoximod significantly suppresses the activity of α-SMA-expressing human cardiac myofibroblasts (hCMs) and promotes apoptosis by up-regulating the genes IRF-1, Fas, and FasL. Moreover, this co-treatment effectively improves cardiac fibrosis[1].