LMK-235

製品コードS7569 バッチS756901

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₂₂N₂O₄

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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	LMK-235は、HDAC4およびHDAC5の選択的阻害剤であり、それぞれのIC50は11.9 nMおよび4.2 nMです。
in vitro	LMK-235 causes HDAC inhibition with IC50 of <1 μM in human cancer cell lines with different sensitivity. In breast cancer cell line MDA-MB-231, tongue cancer cell line Cal27, and esophagus cell line Kyse510 cell line, this compound displays a high cytotoxicity, and markedly enhances the cytotoxicity. In addition, this chemical also shows nanomolar activity against multiple malaria parasite life cycle stages.
in vivo	LMK-235 is a selective inhibitor of HDAC4.

製品説明

LMK-235は、HDAC4およびHDAC5の選択的阻害剤であり、それぞれのIC50は11.9 nMおよび4.2 nMです。

in vitro

LMK-235 causes HDAC inhibition with IC50 of <1 μM in human cancer cell lines with different sensitivity. In breast cancer cell line MDA-MB-231, tongue cancer cell line Cal27, and esophagus cell line Kyse510 cell line, this compound displays a high cytotoxicity, and markedly enhances the cytotoxicity.

In addition, this chemical also shows nanomolar activity against multiple malaria parasite life cycle stages.

in vivo

LMK-235 is a selective inhibitor of HDAC4.

プロトコル(参考用のみ)

キナーゼアッセイ	HDAC IC50 Profiling
キナーゼアッセイ	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 is 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.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/23252603/
https://pubmed.ncbi.nlm.nih.gov/24904967/
https://pubmed.ncbi.nlm.nih.gov/32550904/

カスタマーフィードバック

: 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]

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：

Elastin as a Novel Extracellular Matrix From Aberrant HDAC4 Expression in PDGF-BB-Induced Orbital Fibroblasts From Graves' Ophthalmopathy Patients [ Invest Ophthalmol Vis Sci, 2025, 66(9):30]	PubMed: 40643339
Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5]	PubMed: 38823394
Silica's silent threat: Contributing to skin fibrosis in systemic sclerosis by targeting the HDAC4/Smad2/3 pathway [ Environ Pollut, 2024, 355:124194]	PubMed: 38782158
PTGER4 signaling regulates class IIa HDAC function and SPINK4 mRNA levels in rectal epithelial cells [ Cell Commun Signal, 2024, 22(1):493]	PubMed: 39396982
A COMPARATIVE ANALYSIS TO DETERMINE THE OPTIMUM HISTONE DEACETYLASE INHIBITORS AND ADMINISTRATION ROUTE FOR IMPROVING SURVIVAL AND ORGAN INJURY IN RATS AFTER HEMORRHAGIC SHOCK [ Shock, 2023, 60(1):75-83]	PubMed: 37141162
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

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。