Molecular Weight(MW): 446.5
CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
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Effect of HDAC6 inhibitors on EGFR signaling and sorafenib-mediated EGFR stabilization and activation. a, b A549 and H460 cells were treated with different doses of CAY10603 (a) or ACY1215 (b) for 48 h and then phosphorylated, and total protein levels were evaluated by western blotting. c, d H460 cells were treated with 0.5 μM sorafenib alone or in combination with 0.05 μM CAY10603 (c) or 1 μM ACY1215 (d) for 48 h and then phosphorylated, and total protein levels were evaluated by western blotting.
Med Oncol, 2016, 33(5):50.. CAY10603 purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.|
CAY10603, via inhibition of HDAC6, shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of <1 μM, which can be used as a new molecular probe in exploring HDAC biology. 
HDAC Inhibition Assays:Purified HDACs are incubated with 1 mM carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25 °C in HDAC assay buffer containing 100 mM HEPES (pH 7.5), 25 mM KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model: ((A+((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve. The standard errors of the IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the formula xf4_FitResultStdError.
|In vitro||DMSO||89 mg/mL (199.32 mM)|
|Ethanol||5 mg/mL warmed (11.19 mM)|
|In vivo||5% DMSO+50% PEG 300+ddH2O||9mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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