Name: Piceatannol
Brand: Selleck Chemicals
SKU: S3026
Availability: InStock
Rating: 5 (36 reviews)

Jump to

Quality Control

Batch: Purity: 99.80%

99.80

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other Syk Inhibitors	R406 R406 (free base) PRT062607 (P505-15) HCl Entospletinib (GS-9973) BAY 61-3606 dihydrochloride PRT-060318 2HCl TAK-659 Hydrochloride Lanraplenib (GS-SYK) RO9021 R112

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
human lung mast cells	Function assay			Inhibition of SYK in human lung mast cells assessed as reduction in anti-IgE-stimulated histamine release, EC50=25 μM
human A2780 cells	Proliferation assay		2 days	Antiproliferative activity against human A2780 cells after 2 days by Alamar Blue assay, IC50=41 μM
mouse 3T3L1 cells	Function assay	10 to 50 μM	48 h	Reduction in triglyceride level in mouse 3T3L1 cells at 10 to 50 uM after 48 hrs
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (196.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (16.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	244.24	Formula	C₁₄H₁₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	10083-24-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Astringenin			Smiles	C1=CC(=C(C=C1C=CC2=CC(=CC(=C2)O)O)O)O

Mechanism of Action

Targets/IC₅₀/Ki	Syk (Cell-free assay) Lyn (Cell-free assay) cAK (Cell-free assay) 3 μM PKC (Cell-free assay) 8 μM MLCK (Cell-free assay) 12 μM CDPK (Cell-free assay) 19 μM
In vitro	Piceatannol displays ~10-fold selectivity for Syk over Lyn. This compound treatment in RBL-2H3 cells strongly inhibits the antigen-stimulated phosphorylation of Syk and of most other cellular proteins but not the receptor β or γ subunit, in a dose-dependent manner. It is also a potent inhibitor of histamine release in mast cells. Selective inhibition of Syk by this chemical blocks receptor-mediated down-stream cellular responses in mast cells including prevention of 1,4,5-IP₃ synthesis, secretion and membrane ruffling and spreading. This compound also potently inhibits PKA, PKC, MLCK, and CDPK with IC50 of 3 μM, 8 μM, 12 μM, and 19 μM, respectively. It selectively prevents the IFNα-induced tyrosine phosphorylation of STAT3 and -5 but not STAT1 and -2, paralleled by the loss of Jak1 and IFNAR1 tyrosine phosphorylation but not Tyk2 and IFNAR2. This chemical potently induces apoptotic cell death in BJAB Burkitt-like lymphoma cells with ED50 of 25 μM, through the activation of caspase-3 and mitochondrial permeability transition independent of the CD95/Fas signaling pathway. It inhibits NF-κB activation induced by TNF, H₂O₂, PMA, LPS, okadaic acid, and ceramide. This compound suppresses the expression of TNF-induced NF-κB-dependent reporter gene and of matrix metalloprotease-9, cyclooxygenase-2, and cyclin D1 independent of Syk kinase, by blocking TNF-induced IκBα phosphorylation, p65 phosphorylation, p65 nuclear translocation, and IκBα kinase activation. It directly binds with PI3K in an ATP-competitive manner, and suppresses PI3K activity with anti-atherosclerotic effects more effectively than resveratrol. This chemical inhibits androgen-dependent (AD) and androgen-independent (AI) CaP cell proliferation, which is accompanied by reduced expression of mTOR and its key effectors AKT and eIF4EBP-1.
Kinase Assay	In Vitro Protein-tyrosine Kinase Assays
Kinase Assay	Recombinant Syk is expressed in baculovirus-infected St9 cells. Assays of recombinant Syk activity are carried out using angiotensin I peptide as substrate. The enzyme activities of recombinant Syk are measured by phosphorylation of angiotensin I peptide in the presence of various concentrations of this compound.
In vivo	Oral administration of Piceatannol induces a remarkable amelioration of the disruption of the colonic architecture, a significant reduction in colonic myeloperoxidase (MPO) activity, and a decrease in production of inflammatory mediators such as nitric oxide (NO), prostaglandin (PG) E2, and pro-inflammatory cytokines in BALB/c mice with dextran sulfate sodium (DSS)-induced colitis. This compound treatment inhibits the rises in blood glucose levels at early stages and improves the impaired glucose tolerance at late stages in type 2 diabetic model db/db mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7961959/ [2] https://pubmed.ncbi.nlm.nih.gov/9581512/ [3] https://pubmed.ncbi.nlm.nih.gov/10777558/ [4] https://pubmed.ncbi.nlm.nih.gov/11681415/ [5] https://pubmed.ncbi.nlm.nih.gov/12444159/ [6] https://pubmed.ncbi.nlm.nih.gov/12490796/ [7] https://pubmed.ncbi.nlm.nih.gov/18773974/ [8] https://pubmed.ncbi.nlm.nih.gov/19887493/ [9] https://pubmed.ncbi.nlm.nih.gov/22579688/ [10] https://pubmed.ncbi.nlm.nih.gov/22567414/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Piceatannol Syk inhibitor

Chemical Structure

Molecular Weight: 244.24