ZM 449829

ZM 449829 is a degradation product of ZM 39923 (Item No. 16729) and an inhibitor of JAK3 (IC₅₀ = 0.158 µM).^1,2 It is selective for JAK3 over EGFR and JAK1 (IC₅₀s = 10 and 19.95 µM, respectively) but does inhibit human tissue transglutaminase 2 (TGM2) and transglutaminase factor XIIIa (FXIIIa; IC₅₀s = 0.005 and 0.006 µM, respectively).^1,3 ZM 449829 decreases the formation of cancer stem cells (CSC) within MCF-7-derived mammospheres.⁴ It decreases migration of, and colony formation by, MCF-7 cells when used at a concentration of 10 µM. ZM 449829 (10 µM) also inhibits formation of replication vacuoles in C. burnetii-infected HeLa and THP-1 cells.⁵

WARNING This product is not for human or veterinary use.

1. Brown, G.R., Bamford, A.M., Bowyer, J., et al. Naphthyl ketones: A new class of Janus kinase 3 inhibitors. Bioorg. Med. Chem. Lett. 10(6), 575-579 (2000).

2. Luo, C., and Laaja, P. Inhibitors of JAKs/STATs and the kinases: A possible new cluster of drugs. Drug Discov. Today 9(6), 268-275 (2004).

3. Lai, T.-S., Liu, Y., Tucker, T., et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem. Biol. 15(9), 969-978 (2008).

4. Choi, H.S., Kim, D.-A., Chung, H., et al. Screening of breast cancer stem cell inhibitors using a protein kinase inhibitor library. Cancer Cell Int. 17, 25 (2017).

5. Hussain, S.K., Broederdorf, L.J., Sharma, U.M., et al. Host kinase activity is required for Coxiella burnetii parasitophorous vacuole formation. Front. Microbiol. 1, 137 (2010).