BAY 61-3606  is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (K_i = 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. BAY 61-3606 has been shown to inhibit Syk-mediated cellular functions such as inhibition of high glucose-tyrosine phosphorylation of I κ B α and p65 nuclear translocation. In mast cells BAY 61-3606 has inhibited cytokine synthesis, lipid mediation and degranulation. In addition, monocyte and eosinophil activation by B cells and Fc receptors were suppressed by BAY 61-3606.

An imidazopyrimidine inhibitor of Syk and Syk-mediated functions

≥98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Syk Inhibitor IV

yellow

DMSO : 10 mM

Syk

BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF.

Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats.