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Purity: =100%
CAY10603 is a novel, potent and selective HDAC6 (Histone deacetylase) inhibitor with potential anticancer activity and a potential to treat neurodegenerative diseases. It showed >200-fold selectivity over other HDACs and inhibits HDAC6 with an IC50 of 2 pM. The IC50 values of CAY10603 for HDAC1, 2, 3, 8, and 10 are 271 nM, 252 nM, 0.42 nM, 6851 nM, and 90.7 nM, in that order. For pancreatic cancer cell lines, CAY10603 exhibits strong antiproliferative activity with an IC50 of less than 1 μM. For researching HDAC biology, it might be a helpful chemical probe. Lung adenocarcinoma cell proliferation was inhibited and apoptosis was induced by CAY10603's inhibition of HDAC6. The EGFR signaling pathway was not activated when CAY10603 reduced the amounts of EGFR protein. Furthermore, CAY10603 and gefitinib worked together to destabilize EGFR, which caused the lung adenocarcinoma cell lines to undergo apoptosis. All of our findings point to the possibility that inhibiting HDAC6 could be a successful treatment method for lung adenocarcinoma.
| Targets |
HDAC6 ( IC50 = 0.002 nM ); HDAC3 ( IC50 = 0.42 nM ); HDAC10 ( IC50 = 90.7 nM ); HDAC2 ( IC50 = 252 nM ); HDAC1 ( IC50 = 271 nM ); HDAC8 ( IC50 = 6851 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The acetylated peptide substrate and test compound, labeled with 1 mm carboxyfluorescein (FAM), are incubated with purified HDACs for 17 hours at 25°C in an HDAC assay buffer that contains 100 mm HEPES (pH 7.5), 25 mm KCl, 0.1% BSA, and 0.01% Triton X-100. The addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05% ends the reaction. Using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2), the substrate and product are separated electrophoretically. The Caliper system's Well Analyzer software is used to calculate the fluorescence intensity in the substrate and product peaks. For every sample, the reactions are carried out in duplicate. The XLFit 4-Parameter Logistic Model (sigmoidal dose-response model) and the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel are used to automatically calculate IC50 values: ((A+ ((B_A)/1+((C/x)D)))), where x is the compound concentration, A and B denote the estimated minimum and maximum percent inhibition, respectively, C is the sigmoidal curve's inflection point, and D is its hill slope.
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| Cell Assay |
The ATCC provides the pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86. The cell lines are cultured in DMEM or RPMI medium supplemented with 10% fetal calf serum and l-glutamine. In six wells of a 96-well microtiter plate, duplicate pancreatic cancer cells are plated out at a density of 2.5–4P103 cells per well. Individual wells are treated with diluent (DMSO), different concentrations of SAHA, or the specified HDACIs at a concentration of 1 nm to 50 mm four hours after plating. The colorimetric MTT assay is used to measure cytotoxicity at time "0" and 72 hours after treatment. XLfit is used to compute the IC50 values.
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| References |
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| Molecular Formula |
C22H30N4O6
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| Molecular Weight |
446.5
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| Exact Mass |
446.22
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| Elemental Analysis |
C, 59.18; H, 6.77; N, 12.55; O, 21.50
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| CAS # |
1045792-66-2
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO
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| InChi Key |
WWGBHDIHIVGYLZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H30N4O6/c1-22(2,3)31-21(29)24-16-11-9-15(10-12-16)18-14-17(26-32-18)20(28)23-13-7-5-4-6-8-19(27)25-30/h9-12,14,30H,4-8,13H2,1-3H3,(H,23,28)(H,24,29)(H,25,27)
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| Chemical Name |
tert-butyl N-[4-[3-[[7-(hydroxyamino)-7-oxoheptyl]carbamoyl]-1,2-oxazol-5-yl]phenyl]carbamate
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| Synonyms |
CAY-10603; CAY10603; CAY 10603
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2396 mL | 11.1982 mL | 22.3964 mL | |
| 5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | |
| 10 mM | 0.2240 mL | 1.1198 mL | 2.2396 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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