RO9021

RO9021 is an inhibitor of spleen tyrosine kinase (Syk; IC₅₀ = 5.6 nM).¹ It is selective for Syk over a panel of 392 other kinases at 1 µM. RO9021 also inhibits M. tuberculosis serine/threonine protein kinase G (PknG; IC₅₀ = 4.4 µM).² It inhibits the proliferation of, and induces apoptosis in, primary acute myeloid leukemia (AML) cells when used at a concentration of 5 µM.³ RO0921 prevents RANKL- and M-CSF-induced osteoclastogenesis in isolated mouse bone marrow-derived macrophages (BMDMs; IC₅₀ = 145 nM).¹ It reduces disease severity in a mouse model of collagen-induced arthritis when administered at doses of 5 or 45 mg/kg.

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1. Liao, C., Hsu, J., Kim, Y., et al. Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: Implications for SYK inhibitors in autoimmune disease therapy. Arthirits Res. Ther. 15(5), R146 (2013).

2. Arica-Sosa, A., Alcántara, R., Jiménez-Avalos, G., et al. Identifying RO9021 as a potential inhibitor of PknG from Mycobacterium tuberculosis: Combinative computational and in vitro studies. ACS Omega 7(23), 20204-20218 (2022).

3. Brattås, M.K., Henmsing, A.L., Rye, K.P., et al. Heterogeneity of patient-derived acute myeloid leukemia cells subjected to SYK in vitro inhibition. Int. J. Mol. Sci. 23(23), 14706 (2022).