TDO2-IN-1 

TDO2-IN-1 is a selective TDO2 inhibitor. TDO2-IN-1 binds to the active pocket, heme-binding pocket and substrate-binding pocket of apo-TDO2, interacts with key residues, competitively inhibits heme insertion, and suppresses intracellular TDO2 activity. TDO2-IN-1 can be used in research related to cancer, metabolism and other fields^[1].

TDO2-IN-1 (compound 2) (0.5 nM-10 µM; 24 h) potently inhibits cellular TDO2 activity in SW48 cells, with an IC₅₀ of 14.8 nM, and shows no cytotoxicity at concentrations up to 10 µM^[1].
TDO2-IN-1 (0.5 nM-10 µM; 24 h) does not inhibit IDO1 activity in IFNγ-stimulated SKOV3 cells, with an IC₅₀ greater than 10 µM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

532.63

C₃₀H₃₆N₄O₅

O=C1N2C(C(N([C@@H](C)C3=CC=CC=C3)C(NC4=CC=CC=C4C(C)C)=O)CCC2)=NC(OC)=C1C(OCC)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lotz-Jenne C, et al. Discovery and binding mode of small molecule inhibitors of the apo form of human TDO2. Sci Rep. 2024;14(1):27937. Published 2024 Nov 14.  [Content Brief]