Santacruzamate A (CAY10683)

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

Santacruzamate A (CAY10683) Chemical Structure

Santacruzamate A (CAY10683) Chemical Structure

CAS No. 1477949-42-0

Purity & Quality Control

Santacruzamate A (CAY10683) Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cell Cytotoxicity assay 96 h Cytotoxicity against human HCT116 cells after 96 hrs by MTS-PMS assay, GI50=29.4 μM 24164245
HUT78 cell Cytotoxicity assay 72 h Cytotoxicity against human HUT78 cells after 72 hrs by MTS-PMS assay, GI50=1.4 μM 24164245
Click to View More Cell Line Experimental Data

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]
119 pM
In vitro
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]

Kinase Assay 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 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.

In Vivo
In vivo

Santacruzamate A (CAY10683) is a potent and selective HDAC2 inhibitor that suppressed metastasis in mice liver metastasis model.

Chemical Information & Solubility

Molecular Weight 278.35 Formula

C15H22N2O3

CAS No. 1477949-42-0 SDF Download Santacruzamate A (CAY10683) SDF
Smiles CCOC(=O)NCCCC(=O)NCCC1=CC=CC=C1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (201.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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