CAY10603
For research use only.
Catalog No.S7596 Synonyms: BML-281
14 publications
CAS No. 1045792-66-2
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
4 Customer Reviews
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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.
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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.
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(C) Western blot analysis of a panel of anti-apoptotic and pro-apoptotic proteins in samples treated with different doses of CAY10603.
Oncol Rep, 2016, 36(1):589-97. CAY10603 purchased from Selleck.
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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.
Purity & Quality Control
Choose Selective HDAC Inhibitors
Biological Activity
| Description | CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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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. |
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| Cell Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 89 mg/mL (199.32 mM) |
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| Water | Insoluble | |
| Ethanol | '5 mg/mL warmed | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+50% PEG 300+ddH2O For best results, use promptly after mixing. |
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 |
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| Formula | C22H30N4O6 |
| CAS No. | 1045792-66-2 |
| Storage |
powder in solvent |
| Synonyms | BML-281 |
| Smiles | CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*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
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 )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
I want to use CAY10603 and Tubastatin A via IP for mice. What can serve as the working solution instead of DMSO?
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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.
