EPZ020411 hydrochloride 是一种选择性的PRMT6抑制剂，其IC50值为 10 nM，比作用于 PRMT1 和 PRMT8 选择性高 10 倍多。EPZ020411 hydrochloride 可用于癌症的研究。
| 生物活性 | EPZ020411 hydrochloride is a selective inhibitor ofPRMT6with anIC50of 10 nM, it has >10 folds selectivity forPRMT6overPRMT1andPRMT8. EPZ020411 hydrochloride can be used for the research ofcancer[1][2]. |
| IC50& Target | PRMT6 0.01 μM (IC50) | PRMT1 0.119 μM (IC50) | PRMT8 0.223 μM (IC50) |
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体外研究
(In Vitro) | EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].
Western Blot Analysis[1] | Cell Line: | A375 cells | | Concentration: | 0-20 μM | | Incubation Time: | 24 hours | | Result: | Dose-dependently decreased H3R2 methylation in A375 cells with an IC50of 0.634 μM. |
Cell Viability Assay[2] | Cell Line: | Cultured cochleae cells | | Concentration: | 20 and 40 μM | | Incubation Time: | 6 hours | | Result: | Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells
of the cochlear explants after pretreatment deposed. Reduced hair cell loss caused by cisplatin treatment. |
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体内研究
(In Vivo) | EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2]. 1.19Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats[1]. | Rats
IV 1 mg/kg | Rats
SC 5 mg/kg | | CL (mL/min/kg) | 19.7±1.0 | | | Vss(L/kg) | 11.1±1.6 | | | t1/2(h) | 8.54±1.43 | 9.19±1.60 | | tmax(h) | | 0.444 | | Cmax(ng/mL) | | 844±306 | | AUC0-τ(h·ng/mL) | 745±34 | 2456±135 | | AUC0-inf(h·ng/mL) | 846±45 | 2775±181 | | F (%) | | 65.6±4.3 |
| Animal Model: | C57BL/6J wild-type mice at P28 with acute ototoxicity model[2] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; 10 mg/kg once | | Result: | Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: 0.1 M HCL : 50 mg/mL(104.37 mM;ultrasonic and warming and adjust pH to 2 with HCl and heat to 60℃) DMSO : 50 mg/mL(104.37 mM;Need ultrasonic) H2O : 20 mg/mL(41.75 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.0874 mL | 10.4371 mL | 20.8742 mL | | 5 mM | 0.4175 mL | 2.0874 mL | 4.1748 mL | | 10 mM | 0.2087 mL | 1.0437 mL | 2.0874 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 25 mg/mL (52.19 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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