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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3 Customer Reviews

  • U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.

    Cancer Lett, 2016, 379(1):134-42. CAY10603 purchased from Selleck.

    HPAECs were pre-treated with CAY10603 (CAY, 0.1 μM) for 6 h, then challenged with TNFα (20 ng/ml) for 18 h. Cells were divided into 4 groups: Control (Con), TNF-α alone (TNFα), CAY10603 alone (CAY), and TNF-α+CAY10603 (TNFα+CAY). Representative blots and densitometry analysis of cleaved caspase-3. *P < 0.05 versus TNF-α group, n = 3.

    Oncotarget, 2016, 7(34):54714-54722. CAY10603 purchased from Selleck.

  • 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.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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]
(Cell-free assay)
2 pM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Panc04.03 cells NXPzc4tsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWO3NkBp MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCjbnOwOE4xOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNUDPxE1? MVuxPFY1Ojh7Mh?=
human MiaPaca2 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 MlG0O|IhcA>? MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2rYWDhZ4EzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xJO69VQ>? NVjZXnQxOTh4NEK4PVI>
human HupT3 cells M{DsVHBzd2yrZnXyZZRqd25iYYPzZZk> M3P0dVczKGh? NFmzVpJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFj1dHQ{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zJO69VQ>? M1O1b|E5PjR{OEmy
HPDE 6c7 cells M2nWdGN6fG:2b4jpZ4l1gSCjc4PhfS=> MmLQO|IhcA>? NXfCdYtxS3m2b4TvfIlkcXS7IHHnZYlve3RiSGDESUA3[zdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlUh|ryP M4HGR|E5PjR{OEmy
human SU.86.86 cells NF3t[2lRem:uaX\ldoF1cW:wIHHzd4F6 MVy3NkBp NX23S|dvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWU45Pi56NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPiEQvF2= MUWxPFY1Ojh7Mh?=
human BxPC3 cells MkPHVJJwdGmoZYLheIlwdiCjc4PhfS=> M3TRRlczKGh? NGnze2xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFL4VGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MTFOwG0> M3;WUlE5PjR{OEmy
HMEC MVLDfZRwfG:6aXPpeJkh[XO|YYm= NGW5ZVQ4OiCq MofGR5l1d3SxeHnjbZR6KGGpYXnud5QhUE2HQzDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFizszN NEHmOoQyQDZ2Mki5Ni=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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 Insoluble
In vivo Add solvents individually and in order:
5% DMSO+50% PEG 300+ddH2O
9mg/mL

* 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
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

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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

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

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Frequently Asked Questions

  • Question 1:

    I want to use CAY10603 and Tubastatin A via IP for mice. What can serve as the working solution instead of DMSO?

  • Answer:

    S7596 CAY10603 can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 9mg/ml as a clear solution. The dissolving protocol is the same as S8049.

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID