574711
Syk Inhibitor
The Spleen Tyrosine Kinase Inhibitor, also referenced under CAS 622387-85-3, controls the biological activity of Spleen Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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Synonym(s):
Syk Inhibitor, Spleen Tyrosine Kinase Inhibitor, 3-(1-Methyl-1H-indol-3-yl-methylene)-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Empirical Formula (Hill Notation):
C18H15N3O3S
Recommended Products
Quality Level
Assay
≥97% (sum of two isomers, HPLC)
form
solid
potency
14 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
deep orange
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C18H15N3O3S/c1-21-10-11(13-4-2-3-5-17(13)21)8-15-14-9-12(25(19,23)24)6-7-16(14)20-18(15)22/h2-10H,1H3,(H,20,22)(H2,19,23,24)
InChI key
MLKHXLFEYOOYEY-UHFFFAOYSA-N
General description
A cell-permeable oxindole compound that acts as a potent, reversible, and ATP-competitive Syk inhibitor (IC50 = 14 nM). Has been shown to effectively inhibit FcεRI-mediated degranulation in the rat basophilic leukemia cell line, RBL-2H3 (EC50 = 313 nM).
A cell-permeable, potent, reversible, and ATP-competitive Spleen Tyrosine Kinase (Syk) inhibitor (IC50 = 14 nM). Shown to effectively inhibit FcεRI-mediated degranulation in the rat basophilic leukemia cell line, RBL-2H3 (EC50 = 313 nM).
Biochem/physiol Actions
Cell permeable: yes
EC50 = 313 nM against FcεRI-mediated degranulation in the rat basophilic leukemia cell line, RBL-2H3
Product competes with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Lai, J.Y.Q., et al. 2003. Bioorg. Med. Chem. Lett.13, 3111.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Tai Yeon Koo et al.
Cell biology international, 37(1), 19-28 (2013-01-16)
Atherosclerosis develops from cascades of inflammatory processes. Spleen tyrosine kinase (Syk) and monocyte chemotatic protein-1 (MCP-1) play important roles in the pathogenesis of atherosclerosis. Mycophenolic acid (MPA) has an anti-inflammatory effect. We have investigated whether MPA regulates Syk to repress
Lin Wang et al.
Nature genetics, 53(4), 500-510 (2021-03-31)
Spleen tyrosine kinase (SYK) is a critical immune signaling molecule and therapeutic target. We identified damaging monoallelic SYK variants in six patients with immune deficiency, multi-organ inflammatory disease such as colitis, arthritis and dermatitis, and diffuse large B cell lymphomas.
Genome-Wide Association Study Reveals CLEC7A and PROM1 as Potential Regulators of Paracoccidioides brasiliensis-Induction of Cytokine Production in Peripheral Blood Mononuclear Cells.
de Figueiredo, et al.
Journal of Fungi, 9 (2023)
Omar Rafael Alemán et al.
Frontiers in immunology, 12, 657393-657393 (2021-06-01)
Human neutrophils express two unique antibody receptors for IgG, the FcγRIIa and the FcγRIIIb. FcγRIIa contains an immunoreceptor tyrosine-based activation motif (ITAM) sequence within its cytoplasmic tail, which is important for initiating signaling. In contrast, FcγRIIIb is a glycosylphosphatidylinositol (GPI)-linked
Jung-Yeon Yoo et al.
Cell reports, 33(3), 108245-108245 (2020-10-22)
Cytosolic proteins are required for regulation of NADPH (nicotinamide adenine dinucleotide phosphate) oxidase (Nox) isozymes. Here we show that Src homology 3 (SH3) domain-containing YSC84-like 1 (SH3YL1), as a Nox4 cytosolic regulator, mediates lipopolysaccharide (LPS)-induced H2O2 generation, leading to acute
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