Santacruzamate A (CAY10683)

Catalog No.S7595 Batch:S759502

Technical Data

Formula

C₁₅H₂₂N₂O₃

Molecular Weight

278.35

CAS No.

1477949-42-0

Solubility (25°C)*

In vitro

DMSO

56 mg/mL (201.18 mM)

Ethanol

56 mg/mL (201.18 mM)

Water

Insoluble

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

Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O	10.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 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 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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 clarify; 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 25 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
HDAC2 promotes autophagy-associated HCC malignant progression by transcriptionally activating LAPTM4B [ Cell Death Dis, 2024, 15(8):593]	PubMed: 39147759
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

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SHIPPING AND STORAGE
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