| Bioactivity | R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis[1]. | ||||||||||||
| Target | IC50: 226 nM (Syk kinase) | ||||||||||||
| Invitro | R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC50s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC50 value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC50s of 0.115, 2.01, 1.58 and 1.75 μM, respectively[1].R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | R112 | ||||||||||||
| CAS | 575474-82-7 | ||||||||||||
| Formula | C16H13FN4O2 | ||||||||||||
| Molar Mass | 312.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Rossi AB, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-755. |