LMK-235

製品コードS7569 バッチS756902

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	59 mg/mL (200.44 mM)
		Ethanol	59 mg/mL (200.44 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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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.

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.

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.

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 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.
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

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：

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。

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