8-Nitrotryptanthrin

8-Nitrotryptanthrin is a derivative of tryptanthrin (Item No. 17913) with diverse biological activities.^1,2,3,4,5 It inhibits human recombinant indoleamine 2,3-dioxygenase 1 (IDO1; IC₅₀ = 0.103 μM) and its enzyme activity in HEK293 cells expressing human IDO1 (IC₅₀ = 0.18 μM).¹ 8-Nitrotryptanthrin inhibits the growth of U251 glioblastoma, H522 lung, M14 melanoma, DU145 prostate, and A498 renal cancer cells (GI₅₀s = 4.5, 4.8, 15, 8, and 2 μM, respectively).² It is active against M. tuberculosis, methicillin resistant S. aureus (MRSA), and M. furfur (MICs = 0.032, 0.5, and 5 μg/ml, respectively).^3,4 8-Nitrotyrptanthrin is also active against T. brucei (EC₅₀ = 0.24 μg/ml).⁵

WARNING This product is not for human or veterinary use.

1. Yang, S., Li, X., Hu, F., et al. Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. J. Med. Chem. 56(21), 8321-8331 (2013).

2. Sharma, V.M., Prasanna, P., Seshu, K.V., et al. Novel indolo[2,1-b]quinazoline analogues as cytostatic agents: Synthesis, biological evaluation and structure-activity relationship. Bioorg. Med. Chem. Lett. 12(17), 2303-2307 (2002).

3. Hwang, J.-M., Oh, T., Kaneko, T., et al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J. Nat. Prod. 76(3), 354-367 (2013).

4. Kawakami, J., Matsushima, N., Ogawa, O., et al. Antibacterial and antifungal activities of tryptanthrin derivatives. Trans. Mater. Res. Soc. Jpn. 36(4), 603-606 (2011).

5. Scovill, J., Blank, E., Konnick, M., et al. Antitrypanosomal activities of tryptanthrins. Antimicrob. Agents Chemother. 46(3), 882-883 (2002).