Santacruzamate A (CAY10683)

Catalog No.S7595 Batch:S759501

Technical Data

Formula

C₁₅H₂₂N₂O₃

Molecular Weight

278.35

CAS No.

1477949-42-0

Solubility (25°C)*

In vitro

DMSO

55 mg/mL (197.59 mM)

Ethanol

55 mg/mL (197.59 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

In vivo

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

Protocol (from reference)

Kinase Assay:^{^[1]}	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 Assay:^{^[1]}	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.

Kinase Assay:^{^[1]}

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 Assay:^{^[1]}

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.

References

Customer Product Validation

: Data from [Data independently produced by , , Cell Prolif, 2018, doi: 10.1111/cpr.12447]

Selleck's Santacruzamate A (CAY10683) has been cited by 24 publications

Unveiling the role of HP1α-HDAC1-STAT1 axis as a therapeutic target for HP1α-positive intrahepatic cholangiocarcinoma [ J Exp Clin Cancer Res, 2024, 43(1):152]	PubMed: 38812060
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051]	PubMed: 37598220
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051]	PubMed: 37598220
PLEKHG5 is stabilized by HDAC2-related deacetylation and confers sorafenib resistance in hepatocellular carcinoma [ Cell Death Discov, 2023, 9(1):176]	PubMed: 37248230
Aminocoumarin-based heme oxygenase activity fluorescence probe reveals novel aspects of HO-1 regulation [ Research Square, 2023, 10.21203/rs.3.rs-3485680/v1]	PubMed: none
YTHDC1 is downregulated by the YY1/HDAC2 complex and controls the sensitivity of ccRCC to sunitinib by targeting the ANXA1-MAPK pathway [ J Exp Clin Cancer Res, 2022, 41(1):250]	PubMed: 35974388
STING mediates nuclear PD-L1 targeting-induced senescence in cancer cells [ Cell Death Dis, 2022, 13-9:791]	PubMed: 36109513
Acetylation of Checkpoint suppressor 1 enhances its stability and promotes the progression of triple-negative breast cancer [ Cell Death Discov, 2022, 8(1):474]	PubMed: 36450706
Deacetylation mechanism and potential reversal strategy of long QT syndrome on hERG K+ channel under hypoxia [ Biochim Biophys Acta Mol Basis Dis, 2022, 1868(11):166487]	PubMed: 35840042
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer [ Clin Epigenetics, 2022, 14(1):147]	PubMed: 36371227

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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