All AbMole products are for research use only, cannot be used for human consumption.
Piceatannol is a selective Syk inhibitor with IC50 of ~10 μM. Piceatannol is a plant secondary natural product which inhibits the purified thymocyte p40 kinase (the catalytic fragment of Syk), by competing for the peptide or protein substrate binding site with Ki of 15 μM. Piceatannol also inhibits the activity of the p56lck protein-tyrosine kinase in LSTRA cell membranes or intact cells. Piceatannol preferentially inhibits the activity of Syk in comparison to Lyn in in vitro kinase assays. Selective inhibition of Syk by Piceatannol blocks receptor-mediated down-stream cellular responses (inositol 1,4,5-trisphosphate production, secretion, ruffling, and spreading). Piceatannol is a potent inducer of apoptosis in the lymphoma cell line BJAB by causing a concentration-dependent activation of caspase-3 and mitochondrial permeability transition. Piceatannol but not resveratrol is a very efficient inducer of apoptosis in ex vivo assay with leukemic lymphoblasts of 21 patients suffering from childhood lymphoblastic leukemia (ALL). Piceatannol inhibits TNF-induced NF-κB activation and NF-κB-mediated gene expression through suppression of IκBα kinase and p65 phosphorylation. Piceatannol inhibits the growth of colorectal cancer cell lines and arrests Caco-2 cells in the S phase of the cell cycle. Sequential treatment with Piceatannol and Ara-C yields synergistic growth inhibitory effects against HL-60 cells because of remarkably increased Ara-CTP formation after Piceatannol preincubation. Exposure of different-stage PC-3 prostate cancer (CaP) cells to Piceatannol also results in cell-type-specific downregulation of mTOR and its upstream and downstream effector proteins, AKT and eIF-4E-BP1.
| Molecular Weight | 244.24 |
| Formula | C14H12O4 |
| CAS Number | 10083-24-6 |
| Solubility (25°C) | DMSO 28 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Kishore Banik, et al. Piceatannol: A natural stilbene for the prevention and treatment of cancer
[4] Yang Cao, et al. Overview of Cellular Mechanisms and Signaling Pathways of Piceatannol
| Related Syk Products |
|---|
| GSK143
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. |
| PRT062607
PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. |
| GSK143 dihydrochloride
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. |
| Syk Kinase Peptide Substrate
Syk Kinase Peptide Substrate is a Syk kinase peptide substrate. |
| TOP1288
TOP1288 is an SRC/Syk/p38α inhibitor for studies related to ulcerative colitis. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
