R112

• CAT Number: I004144
• CAS Number: 575474-82-7
• Molecular Formula: C16H13FN4O2
• Molecular Weight: 312.304
• Purity: ≥95%
• Target: Syk
• Solubility: DMSO: ≥ 41 mg/mL
• Storage: -20°C
• IC50: 226 nM [1]
• IUPAC Name: 3-[[5-fluoro-2-(3-hydroxyanilino)pyrimidin-4-yl]amino]phenol
• InChI: InChI=1S/C16H13FN4O2/c17-14-9-18-16(20-11-4-2-6-13(23)8-11)21-15(14)19-10-3-1-5-12(22)7-10/h1-9,22-23H,(H2,18,19,20,21)
• InChIKey: TVKGTSHBQZEFEE-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)O)NC2=NC(=NC=C2F)NC3=CC(=CC=C3)O

R112 (CAT: I004144) is an ATP-competitive inhibitor of Syk kinase, a non-receptor tyrosine kinase involved in immune cell signaling. By inhibiting Syk kinase, R112 disrupts downstream signaling events crucial for immune cell activation. This pharmacological activity makes R112 a potential candidate for therapeutic applications in autoimmune diseases and certain cancers. In autoimmune diseases, R112 may help modulate aberrant immune responses and mitigate tissue damage. Additionally, targeting Syk kinase with R112 has been explored as a strategy in certain hematological malignancies. Further research is underway to fully explore the therapeutic potential of R112 as a Syk kinase inhibitor.

Reference

1:Identification of the Syk kinase inhibitor R112 by a human mast cell screen. Rossi AB, Herlaar E, Braselmann S, Huynh S, Taylor V, Frances R, Issakani SD, Argade A, Singh R, Payan DG, Masuda ES.J Allergy Clin Immunol. 2006 Sep;118(3):749-55. Epub 2006 Jul 28. PMID: 16950297 2:Mast cell inhibitor R112 is well tolerated and affects prostaglandin D2 but not other mediators, symptoms, or nasal volumes in a nasal challenge model of allergic rhinitis. Guyer BJ, Shimamoto SR, Bradhurst AL, Grossbard EB, Dreskin SC, Nelson HS.Allergy Asthma Proc. 2006 May-Jun;27(3):208-13. PMID: 16913263 3:An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. Meltzer EO, Berkowitz RB, Grossbard EB.J Allergy Clin Immunol. 2005 Apr;115(4):791-6. PMID: 15806000 4:Apolipoprotein E R112; R251G: a carboxy-terminal variant found in patients with hyperlipidemia and coronary heart disease. Kang AK, Jenkins DJ, Wolever TM, Huff MW, Maguire GF, Connelly PW, Hegele RA.Mutat Res. 1997 Sep;382(1-2):57-65. PMID: 9360638