574712
Syk Inhibitor II
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.
别名:
Syk Inhibitor II, 2-(2-Aminoethylamino)-4-(3-trifluoromethylanilino)-pyrimidine-5-carboxamide, Dihydrochloride, Dihydrate
InChI key
LCACSMNPIITJGG-UHFFFAOYSA-N
InChI
1S/C14H15F3N6O.2ClH.2H2O/c15-14(16,17)8-2-1-3-9(6-8)22-12-10(11(19)24)7-21-13(23-12)20-5-4-18;;;;/h1-3,6-7H,4-5,18H2,(H2,19,24)(H2,20,21,22,23);2*1H;2*1H2
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
off-white
solubility
DMSO: 100 mg/mL, water: 25 mg/mL
shipped in
ambient
Quality Level
General description
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
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
Preparation Note
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
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 1
Kevin Bode et al.
Cell reports, 29(13), 4435-4446 (2019-12-26)
Uptake of apoptotic cells (ACs) by dendritic cells (DCs) and induction of a tolerogenic DC phenotype is an important mechanism for establishing peripheral tolerance to self-antigens. The receptors involved and underlying signaling pathways are not fully understood. Here, we identify Dectin-1 as a
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