Santacruzamate A (CAY10683)

製品コードS7595 バッチS759502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H22N2O3
分子量 278.35 CAS No. 1477949-42-0
Solubility (25°C)* 体外 DMSO 56 mg/mL (201.18 mM)
Ethanol 56 mg/mL (201.18 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 30%PEG300 5%Tween80 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. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 HuT-78 cells, and HCT-116 cells
濃度 ~100 μM
反応時間 72 or 96 hours
実験の流れ

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.
動物実験 動物モデル Female BALB/c nude mice
投薬量 3 mg/kg
投与方法 i.v.

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Porcine Deltacoronavirus Infection Cleaves HDAC2 to Attenuate Its Antiviral Activity [ J Virol, 2022, 96(16):e0102722] PubMed: 35916536

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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