EPZ020411

A PRMT6 inhibitor

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库存: 现货

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数量
1mg

￥687.00

550.00

- +
5mg

￥3075.00

2460.00

- +
10mg

￥5375.00

4300.00

- +
25mg

￥11762.00

9410.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci14446
CAS: 1700663-41-7
别名:
分子式: C25H38N4O3
分子量: 442.59
纯度: >98%
溶解度: DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.3 mg/ml
储存: Store at -20°C
库存: 现货

Background

IC50: 10 nM

EPZ020411 is an inhibitor of PRMT6.

PRMT6, a member of the protein arginine methyltransferasefamily, comprises 45 enzymes. The post-translational modifications of PRMT6 are important regulators of RNA processing, transcriptional regulation, and signal transduction.

In vitro: In biochemical assays, EPZ020411 was found to be over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases, such as PRMT3, PRMT4, PRMT5 and PRMT7. In addition, EPZ020411 treatment led to a dose-dependent decrease in H3R2 methylation, while treatment with its PRMT6-inactive analog did not generate an IC50 at concentrations up to 20 μM [1].

In vivo: Animal study found that male SD rats i.v. administered a single dose of EPZ020411 at 1 mg/kg showed a moderate clearance of 19.7 mL/min/kg, with a volume of distribution at steady state of 11.1 L/kg, and a mean terminal half-life of 8.54 h. Following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 was observed, resulting in EPZ020411 unbound concentration remaining over the PRMT6 IC50 for more than 12 h [1].

Clinical trial: Up to now, EPZ020411 is still in the preclinical development stage.

Reference:
[1] Mitchell LH, et al.? Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659.