| Bioactivity | RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM. | ||||||||||||
| Target | IC50: 5.6 nM (SYK) | ||||||||||||
| Invitro | RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay[1]. | ||||||||||||
| Name | RO9021 | ||||||||||||
| CAS | 1446790-62-0 | ||||||||||||
| Formula | C18H25N7O | ||||||||||||
| Molar Mass | 355.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liao C, 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. |