EPZ020411 hydrochloride

A PRMT6 inhibitor

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库存: 现货

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5mg

￥2175.00

1740.00

- +
10mg

￥3775.00

3020.00

- +
50mg

￥7012.00

5610.00

- +
100mg

￥12287.00

9830.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce56242
CAS: 2070015-25-5
别名:
分子式: C25H39ClN4O3
分子量: 479.06
纯度: >98%
溶解度: DMSO: 50 mg/mL (104.37 mM); Water: ≥ 41 mg/mL (85.58 mM)
储存: Store at 4°C, stored under nitrogen
库存: 现货

Background

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC₅₀ = 10 nM) that less potently targets PRMT1 and PRMT8 (IC₅₀s = 119 and 223 nM, respectively).¹ It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC₅₀ = 0.637 ?M).¹ EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC₅₀ value for more than 12 hours.¹

1.Mitchell, L.H., Drew, A.E., Ribich, S.A., et al.Aryl pyrazoles as potent inhibitors of arginine methyltransferases: Identification of the first PRMT6 tool compoundACS Med. Chem. Lett.6(6)655-659(2015)