The Syk Inhibitor II, also referenced under CAS 227449-73-2, controls the biological activity of Syk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Syk Inhibitor II, 2-(2-Aminoethylamino)-4-(3-trifluoromethylanilino)-pyrimidine-5-carboxamide, Dihydrochloride, Dihydrate
A cell-permeable pyrimidine-carboxamide compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Syk (IC50 = 41 nM), while affecting PKCε, PKCβII, ZAP-70, Btk, and Itk only at much higher concentrations (IC50 = 5.1, 11, 11.2, 15.5, and 22.6 µM, respectively). Inhibits FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and passive cutaneous anaphylaxis (PCA) reaction in mice in vivo (ID50 = 13.2 mg/kg, s.c.).
Biochem/physiol Actions
Cell permeable: yes
Primary Target Syk
Product competes with ATP.
Reversible: yes
Target IC50: 41 nM against Syk; 460 nM against FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Hisamichi, H., et al. 2005. Bioorg. Med. Chem.13, 4936.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
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