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Syk Inhibitor II dihydrochloride

Catalog No. T4391 CAS 227449-73-2

Synonyms: Syk Inhibitor II (hydrochloride)

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor II is a cell-permeable, pyrimidine-carboxamide compound that selectively and reversibly blocks Syk (IC50 = 41 nM) in an ATP-competitive manner. It is much less potent against PKCε, PKCβII, ZAP-70, Btk, and Itk (IC50s = 5.1, 11, 11.2, 15.5, and 22.6 μM, respectively).

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Syk Inhibitor II dihydrochloride Chemical Structure

Syk Inhibitor II dihydrochloride, CAS 227449-73-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 132.00
2 mg	In stock	$ 223.00
5 mg	In stock	$ 479.00
10 mg	In stock	$ 682.00
25 mg	In stock	$ 996.00
50 mg	In stock	$ 1,330.00
100 mg	In stock	$ 1,790.00
1 mL * 10 mM (in DMSO)	In stock	$ 479.00

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Purity: 99.59%

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Description	Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor II is a cell-permeable, pyrimidine-carboxamide compound that selectively and reversibly blocks Syk (IC50 = 41 nM) in an ATP-competitive manner. It is much less potent against PKCε, PKCβII, ZAP-70, Btk, and Itk (IC50s = 5.1, 11, 11.2, 15.5, and 22.6 μM, respectively).
Targets&IC50	BTK:15.5 μM, ZAP70:11.2 μM, PKCε:5.1 μM, PKCβII:11 μM, Syk:41 nM, ITK:22.6 μM
In vitro	Syk inhibitor II has been shown to prevent FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM).
In vivo	Syk inhibitor II has been shown to inhibit passive cutaneous anaphylaxis reactions in mice (ID50 = 13.2 mg/kg, s.c.).
Kinase Assay	A 2 μM portion of DMSO solution of each compound to be tested was added to each well containing 50 ll of a reaction solution [composition: 20–200 ng of recombinant kinase, 50 mM Tris–HCl (pH 7–8), 10 mM MgCl2 or MnCl2, 50 mM NaCl, 1 mM DTT, optimum concentration of the substrate peptide, and 0.1 lCi [c 33P]ATP (10 mCi/mL, Amersham)]. This was prepared in OptiplateTM (PACKARD) and allowed to stand at room temperature for 1 h to effect tyrosine phosphorylation. The reaction was terminated by adding PBS containing 0.25 mg SPA beads, 50 lM ATP, 5 mM EDTA, and 1% Triton X-100 in an amount of 150 ll per well. The plate was sealed, stirred, allowed to stand at room temperature for 15 min, and then centrifuged at 1500 rpm for 3 min to effect precipitation of the SPA beads. Radioactivity of each well was measured using TOP COUNT (PACKARD), and the tyrosine phosphorylation activity by the kinases was calculated. They are for reference only.
Animal Research	ICR mice were passively sensitized by subcutaneously injectinganti-dinitrophenyl (DNP)-coupled IgE under the right ear pinna, while lightly anesthetizing with ether. After 24hr, each mouse was challenged by injecting amixture of DNP-conjugated bovine serum albumin and 200 μl of 0.5% Evans blue solution via the tail vein to induce passive cutaneous anaphylaxis. Thirty minutes after the challenge, the mice were sacrificed to take both ears and the amount of dye from the blueing region was measured. Test compounds or vehicle alone as a control were subcutaneously administered to the mice 30 minbefore the antigen challenge. The dye in the tissues was extracted with formamide and colorimetrically determined at 620 nm. A value obtained by subtracting the dye content of the left ear from the dye content of the right ear was used as the amount of dye leaked into the tissues by the PCA reaction.

Synonyms	Syk Inhibitor II (hydrochloride)
Molecular Weight	413.22
Formula	C14H17Cl2F3N6O
CAS No.	227449-73-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

PBS(pH7.2): 10 mg/mL

Ethanol: 0.3 mg/mL

DMSO: 30 mg/mL

References and Literature

1. Hisamichi H, etal. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives[J]. Bioorganic & medicinal chemistry, 2005, 13(16): 4936-4951.

Related compound libraries

This product is contained In the following compound libraries：

TGF-beta/Smad Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Angiogenesis related Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Immuno-Oncology Compound Library Bioactive Compound Library

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Keywords

Syk Inhibitor II dihydrochloride 227449-73-2 Angiogenesis Chromatin/Epigenetic Cytoskeletal Signaling Others Tyrosine Kinase/Adaptors Syk Tyrosine Kinases PKC BTK Syk Inhibitor II Syk Inhibitor II (hydrochloride) Syk Inhibitor II Dihydrochloride inhibitor inhibit

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