EPZ020411 2HCl

製品コードS7820 バッチS782001

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

C₂₅H₄₀Cl₂N₄O₃

分子量

515.52

CAS No.

2070015-25-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (193.97 mM)

Ethanol

100 mg/mL (193.97 mM)

Water

81 mg/mL (157.12 mM)

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	EPZ020411 は、IC50 が 10 nM の強力で選択的な低分子 PRMT6 阻害剤です。
in vitro	Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). In biochemical assays EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including four arginine methyltransferases (PRMT3, PRMT4, PRMT5, and PRMT7). The compound shows poor permeability in the parallel artificial membrane permeation assay.
in vivo	EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. Male Sprague-Dawley rats administered a single dose of EPZ020411 at 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. Following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 ± 4.3% is observed, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A375 cells
	濃度	0-20 μM
	反応時間	48 h
	実験の流れ	A375 (CRL-1619) cells are cultured in DMEM plus 10% (vol/vol) FBS. PRMT6 is cloned into BamHI and EcoRI sites of a pcDNA4 HisMAX_A plasmid. Transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent according to procedures recommended by the manufacturer. Cells are seeded at 200,000 cells/well in 6-well plates. The following day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence of increasing concentrations of compound up to 20 μM. Cell pellets are collected after 48 hours of compound treatment.
動物実験	動物モデル	Sprague-Dawley rats
	投薬量	1 mg/kg
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/26101569/

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：

PRMT6-mediated ADMA promotes p62 phase separation to form a negative feedback loop in ferroptosis [ Theranostics, 2024, 14(10):4090-4106]	PubMed: 38994016
A mycobacterial effector promotes ferroptosis-dependent pathogenicity and dissemination [ Nat Commun, 2023, 14(1):1430]	PubMed: 36932056
Inhibition of PRMT6 reduces neomycin-induced inner ear hair cell injury through the restraint of FoxG1 arginine methylation [ Inflamm Res, 2022, 71(3):309-320]	PubMed: 35190853
Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. [ Theranostics, 2020, 10(1):133-150]	PubMed: 31903111

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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