R 112

Modify Date: 2024-01-02 19:39:57

R 112 Structure
R 112 structure
Common Name R 112
CAS Number 575474-82-7 Molecular Weight 312.29800
Density N/A Boiling Point N/A
Molecular Formula C16H13FN4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of R 112


R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. IC50 value: 226 nM [1]Target: Sykin vitro: R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1]

 Names

Name 3,3'-[(5-Fluoro-2,4-pyrimidinediyl)diimino]diphenol
Synonym More Synonyms

 R 112 Biological Activity

Description R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. IC50 value: 226 nM [1]Target: Sykin vitro: R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1]
Related Catalog
References

[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.

[2]. Meltzer EO, et al. An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. J Allergy Clin Immunol. 2005 Apr;115(4):791-796.

 Chemical & Physical Properties

Molecular Formula C16H13FN4O2
Molecular Weight 312.29800
Exact Mass 312.10200
PSA 93.53000
LogP 3.00900
Appearance of Characters offwhite solid

 Synonyms

R 112
R112