ido in 5

IDO-IN-5 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).

IDO1-IN-5 is a selective, potent and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

(S)-IDO1-IN-5 is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL(IC50 value less than 1.5 µΜ).

(Rac)-IDO1-IN-5 is a racemate of IDO1-IN-5, a potent, selective, and brain-penetrating inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity. It specifically binds to apo-IDO1, which lacks heme, instead of mature heme-bound IDO1.

IDO-IN-16 (compound 5) is an IDO inhibitor with an IC50 value of 36 nM.

1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.

1. Coptisine chloride (NSC-119754) can be absorbed across intestinal epithelial cells, and completely absorbed compounds.

1. Coptisine sulfate has growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program.