CAY10603 1045792-66-2

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Molecular Weight:

446.5 CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.

Biological Activity

CAY10603, via inhibition of HDAC6, shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of






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.

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.

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Product Categories : Epigenetics > HDAC Inhibitor