CAY10603

Catalog No.S7596

CAY10603 Chemical Structure

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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1 Customer Review

  • 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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Notes:

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.

Biological Activity

Description CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
Targets
HDAC6 [1] HDAC1 [1]
2 pM 271 nM
In vitro

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. [1]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 cells
  • Concentrations: ~50 μM
  • Incubation Time: 72 hours
  • Method: The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nM to 50 mM. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay according to the manufacturer’s suggestions. The IC50 values are calculated using XLfit.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (199.32 mM)
Ethanol 5 mg/mL warmed (11.19 mM)
Water <1 mg/mL
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.

Chemical Information

Molecular Weight 446.5
Formula

C22H30N4O6

CAS No. 1045792-66-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

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.

Handling Instructions

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

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID