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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C15H22N2O4 |
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分子量 | 294.35 | CAS No. | 1418033-25-6 | |
Solubility (25°C)* | 体外 | DMSO | 58 mg/mL (197.04 mM) | |
Ethanol | 58 mg/mL (197.04 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively. |
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in vitro | LMK-235 causes HDAC inhibition with IC50 of <1 μM in human cancer cell lines with different sensitivity towards cisplatin. In breast cancer cell line MDA-MB-231, tongue cancer cell line Cal27, and esophagus cell line Kyse510 cell line, LMK-235 displays a high cytotoxicity, and markedly enhances the cytotoxicity of cisplatin. [1] In addition, LMK-235 also shows nanomolar activity against multiple malaria parasite life cycle stages. [2] |
in vivo | LMK-235 is a selective inhibitor of HDAC4. |
キナーゼアッセイ | HDAC IC50 Profiling | |
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The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company’s standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds. | ||
細胞アッセイ | 細胞株 | A2780, Cal27, Kyse510, and MDA-MB-231 cell lines |
濃度 | ~10 μM | |
反応時間 | 72 hours | |
実験の流れ | The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow MTT to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance s measured at 544 and 690 nm in a FLUOstar microplate reader. |
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動物実験 | 動物モデル | C57BL/6-BALB/c mice |
投薬量 | 20 mg/kg | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Clin Epigenetics, 2018, 10(1):120]
Data from [Data independently produced by , , Oncotarget, 2016, 7(39):63829-63838]
Data from [Data independently produced by , , Oncotarget, 2016, 7(25):37966-37978]
Protective effect of HDACIs in improves survival and organ injury after CLP-induced sepsis [ Surg Open Sci, 2023, 12:35-42] | PubMed: 36936452 |
Kinase signalling in excitatory neurons regulates sleep quantity and depth [ Nature, 2022, 612(7940):512-518] | PubMed: 36477539 |
HDAC5-mediated Smad7 silencing through MEF2A is critical for fibroblast activation and hypertrophic scar formation [ Int J Biol Sci, 2022, 18(15):5724-5739] | PubMed: 36263180 |
Yeast beta-glucan mediates histone deacetylase 5-induced angiogenesis in vascular endothelial cells [ Int J Biol Macromol, 2022, 211:556-567] | PubMed: 35569678 |
Leveraging patient derived models of FGFR2 fusion positive intrahepatic cholangiocarcinoma to identify synergistic therapies [ NPJ Precis Oncol, 2022, 6(1):75] | PubMed: 36274097 |
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 |
HDAC5-Mediated Acetylation of p100 Suppresses Its Processing [ Int Dent J, 2022, S0020-6539(22)00199-X] | PubMed: 36156247 |
CaMKII inhibition protects against hyperthyroid arrhythmias and adverse myocardial remodeling [ Biochem Biophys Res Commun, 2022, 615:136-142] | PubMed: 35617800 |
NADPH levels affect cellular epigenetic state by inhibiting HDAC3-Ncor complex [ Nat Metab, 2021, 3(1):75-89] | PubMed: 33462516 |
Quantitative control of noise in mammalian gene expression by dynamic histone regulation [ Elife, 2021, 10e65654] | PubMed: 34379055 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。