Santacruzamate A (CAY10683)

Catalog No.S7595

Santacruzamate A (CAY10683) Chemical Structure

Molecular Weight(MW): 278.35

Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.
Targets
HDAC2 [1] HDAC6 [1] HDAC4 [1]
119 pM 434 nM >1000 nM
In vitro

Santacruzamate A inhibits the growth of HCT116 colon carcinoma cells and HuT-78 cutaneous T-cell lymphoma cells, with GI50 values of 29.4 μM and 1.4 μM, respectively. However, Santacruzamate A shows hypotoxicity to human dermal fibroblast cells (GI50 >100 μM). [1]

Protocol

Kinase Assay
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HDAC Enzyme Assay:

The commercially availablae human recombinant enzyme and fluorogenic HDAC assay kits have used to measure percent inhibition and IC50 values of three HDAC isozymes (HDAC2, HDAC4, HDAC6). Briefly, the inhibitor is added sequentially to a black, flat-bottom 96-well microtiter plate, and the reaction mixture is incubated for 30 min at 37°C. The potent HDAC inhibitor trichostatin A (included in the assay kit) is added to the bifunctional HDAC assay developer at a final reaction concentration of 1 μM to stop deacetylation and initiate the release of the fluorophore. The reaction mixture is further incubated at room temperature for 15 min. Fluorescence is measured on a Spectra Max Gemini XPS using an excitation wavelength of 360 nm and a detection wavelength of 460 nm.
Cell Research
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  • Cell lines: HuT-78 cells, and HCT-116 cells
  • Concentrations: ~100 μM
  • Incubation Time: 72 or 96 hours
  • Method:

    HuT-78 cells incubated in Iscove’s modified Dulbecco’s medium supplemented with 20% FBS, 1% penicillin/streptomycin, and 1% L-glutamine. HCT-116 cells cultivated using McCoy’s 5A medium supplemented with 10% FBS, 1% penicillin/streptomycin, and 1% nonessential amino acids. Cells were seeded in a 96-well plate at 5000cells per well. Before treatment, the plates were incubated at 37°C, 5% CO2 for 24 h. Treatment with inhibitors were incubated in wells for 72 or 96 h using SAHA as a positive control. Antiproliferative activity was determined using a standard MTS-PMS assay.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL (197.59 mM)
Ethanol 55 mg/mL (197.59 mM)
Water <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* 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 278.35
Formula

C15H22N2O3

CAS No. 1477949-42-0
Storage powder
in solvent
Synonyms N/A

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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

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID