AZ505, inhibitor
AZ505
Purity
98.00%
Synonyms
AZ505; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 40mg/mL (69.26mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C29H38Cl2N4O4
SMILES
OC1=C2NC(=O)COC2=C(CCNCCN(C2CCCCC2)C(=O)CCNCCC2=CC(Cl)=C(Cl)C=C2)C=C1
CAS Number
1035227-43-0
Kinase Assay
SMYD2 is expressed in insect cells and purified. Methylation (12 uL) reactions are carried out in TDT buffer (50mM Tris-HCl [pH 9.0], 2mM DTT, and 0.01% Tween 20) at room temperature using 1.25nM SMYD2 protein, 200nM SAM, and 100nM biotinylated p53 peptide substrate (Biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH) in low volume 384-well plates. Following a 75 min incubation period, reactions are quenched by the addition of 5uL of detection solution (20mM HEPES [pH 7.4], 1.7mg/mL BSA, 340mM NaCl, 680uM SAH, 0.04mg/mL Streptavidin-coated AlphaScreen donor, and Protein A-coated acceptor beads), and 1nM of a custom p53K370me1 polyclonal antibody. Reaction plates are incubated overnight in the dark at room temperature and read using an Envision 2101 Multi-label Reader. Compounds showing >50% inhibition of SMYD2 are nominated for concentration dose-response determination and are also subjected to an artifact assay. Seven compound concentrations are selected beginning at 30uM with six half-log dilution steps. The artifact assay conditions are identical to those in the SMYD2 enzymatic activity assay, except for the absence of SMYD2 protein and the presence of 1nM methylated p53 peptide. IC50 values are calculated from dose-response data using in-house software [2].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Related Product Information for AZ505, inhibitor
AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12uM).
Product Categories/Family for AZ505, inhibitor
References
Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.
Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.
Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYDStructure. 2011 Sep 7;19(9):1262-73.
Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.
Komatsu S, et al. Overexpression of SMYD2 contributes to malignant outcome in gastric cancer. Br J Cancer. 2015 Jan 20;112(2):357-64.
Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYDStructure. 2011 Sep 7;19(9):1262-73.
Ferguson AD, et al. Structural basis of substrate methylation and inhibition of SMYD2. Structure. 2011 Sep 7;19(9):1262-73.
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Product Notes
The AZ505 (Catalog #AAA5764356) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "AZ505, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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