| Name | CAY10603 |
| Description | CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor. |
| Cell Research | 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) |
| Kinase Assay | 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. |
| In vivo | CAY10603 exhibits effective anti-proliferative activity against pancreatic cancer cell lines by inhibiting HDAC6, with an IC50 of less than 1 μM. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 5 mg/mL (11.2 mM), Heating is recommended.
DMSO : 145 mg/mL (324.75 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.39 mM), Sonication is recommended.
|
| Keywords | Inhibitor | inhibit | Histone deacetylases | HDAC6 | HDAC1 | HDAC | CAY-10603 | CAY10603 | CAY 10603 | BML281 | BML 281 |
| Inhibitors Related | Panobinostat | Theophylline monohydrate | Valproic acid sodium salt | Methoxyacetic acid | Sodium 4-phenylbutyrate | Acefylline | Manganese chloride (tetrahydrate) | Curcumin | Valproic Acid | Sodium butanoate | 4-Phenylbutyric acid | Theophylline |
| Related Compound Libraries | Highly Selective Inhibitor Library | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
