EPZ020411 hydrochloride是一种具有高效选择性，且口服生物利用度高的蛋白质精氨酸甲基转移酶6（PRMT6）抑制剂，IC50值为10nM。
Cas No.:2070015-25-5
Sample solution is provided at 25 µL, 10mM.
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EPZ020411 hydrochloride is a highly selective, orally bioavailable inhibitor of protein arginine methyltransferase 6 (PRMT6), with an IC50 value of 10nM[1]. PRMT6 regulates gene expression by catalyzing asymmetric dimethylation of histone H3 at arginine 2 (H3R2) and plays critical roles in stem cell function regulation, proliferation control, and differentiation[2]. EPZ020411 hydrochloride exhibits selectivity for PRMT6 over PRMT1 and PRMT8 and is commonly used in studies of epigenetic regulation, cancer, and hearing loss protection[3,4].
In vitro, treatment of mouse microglial BV2 cells with EPZ020411 hydrochloride (1, 10, 20, 50, 100, 1000μM) for 24h showed that concentrations of 50μM and above significantly inhibited BV2 cell viability[5]. EPZ020411 (10μM) treatment of primary mouse cortical neurons co-overexpressing HTT 548-17Q and EGFP-PRMT6 for 24h reversed the PRMT6 overexpression-induced increase in huntingtin (HTT) arginine methylation levels[6]. EPZ020411 hydrochloride (4μM) treatment of mismatch repair (MMR)-proficient colorectal cancer SW480 cells for 24h significantly attenuated the assembly of MutSα and MutSβ complexes[7].
In vivo, EPZ020411 hydrochloride (10mg/kg; once daily) administered via intraperitoneal injection to BALB/c mice bearing subcutaneous xenografts of microsatellite stable (MSS) murine colorectal cancer CT26 cells for 3 weeks significantly inhibited tumor growth[7].
References:
[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 compound[J]. ACS Medicinal Chemistry Letters, 2015, 6(6): 655-659.
[2] OKUNO K, AKIYAMA Y, SHIMADA S, et al. Asymmetric dimethylation at histone H3 arginine 2 by PRMT6 in gastric cancer progression[J]. Carcinogenesis, 2019, 40(1): 15-26.
[3] WANG J, XIAO Z, LI P, et al. PRMT6-CDC20 facilitates glioblastoma progression via the degradation of CDKN1B[J]. Oncogene, 2023, 42(14): 1088-1100.
[4] LI J, LIU C, QIU S, et al. Epigenetic modifications in sensorineural hearing loss: protective mechanisms and therapeutic potential[J]. Current Medical Science, 2025, 45(3): 415-429.
[5] HUA T, KONG E, ZHANG H, et al. PRMT6 deficiency or inhibition alleviates neuropathic pain by decreasing glycolysis and inflammation in microglia[J]. Brain, Behavior, and Immunity, 2024, 118: 101-114.
[6] MIGAZZI A, SCARAMUZZINO C, ANDERSON E N, et al. Huntingtin-mediated axonal transport requires arginine methylation by PRMT6[J]. Cell Reports, 2021, 35(2).
[7] DUAN J, CHEN T, LI Q, et al. Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer[J]. Journal for ImmunoTherapy of Cancer, 2025, 13(3): e010639.
EPZ020411 hydrochloride是一种具有高效选择性，且口服生物利用度高的蛋白质精氨酸甲基转移酶6（PRMT6）抑制剂，IC50值为10nM[1]。PRMT6通过对组蛋白H3R2进行精氨酸不对称二甲基化来调节基因表达，在调节干细胞功能、增殖控制和分化等方面发挥关键作用[2]。EPZ020411 hydrochloride对PRMT6的选择性远高于PRMT1和PRMT8，通常用于表观遗传调控、癌症和保护听力损失的研究[3,4]。
在体外，EPZ020411 hydrochloride（1, 10, 20, 50, 100, 1000μM）处理小鼠小胶质BV2细胞24h，50μM及以上浓度的EPZ020411 hydrochloride可显著抑制BV2细胞的活力[5]。EPZ020411 hydrochloride（10μM）处理同时过表达了HTT 548-17Q和EGFP-PRMT6的原代小鼠皮层神经元24h，能够逆转PRMT6过表达引起的huntingtin（HTT）蛋白精氨酸甲基化水平升高[6]。EPZ020411 hydrochloride（4μM）处理错配修复（MMR）功能完备的结直肠癌SW480细胞24h，显著减弱了MutSα和MutSβ复合物的组装[7]。
在体内，EPZ020411 hydrochloride（10mg/kg; once daily）通过腹腔注射治疗携带微卫星稳定（MSS）鼠源结直肠癌细胞CT26皮下移植瘤的BALB/c小鼠3周，能够显著抑制肿瘤的生长[7]。
| Cell experiment [1]: | |
Cell lines | MMR-proficient cell line SW480 |
Preparation Method | SW480 cells were treated with 4μM EPZ020411 hydrochloride for 24h, then cells were lysed and immunoprecipitated with an anti-MSH2 antibody, followed by immunoblotting with anti-MSH3 and anti-MSH6 antibodies to assess the assembly of MutSα and MutSβ complexes. |
Reaction Conditions | 4µM; 24h |
Applications | Treatment with EPZ020411 hydrochloride significantly reduced the assembly of the MutSα and MutSβ complexes. |
| Animal experiment [1]: | |
Animal models | BALB/c mice bearing subcutaneous CT26 tumors |
Preparation Method | BALB/c mice bearing subcutaneous CT26 tumors were administered with EPZ020411 hydrochloride (10mg/kg) via intraperitoneal injection once daily for 3 weeks, then tumor weight was examined and calculated. |
Dosage form | 10mg/kg; once daily; 3 weeks; i.p. |
Applications | Treatment with EPZ020411 hydrochloride significantly inhibited tumor growth. |
References: | |
| Cas No. | 2070015-25-5 | SDF | |
| Canonical SMILES | CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2.Cl[H] | ||
| 分子式 | C25H39ClN4O3 | 分子量 | 479.06 |
| 溶解度 | DMSO: 50 mg/mL (104.37 mM); Water: ≥ 41 mg/mL (85.58 mM) | 储存条件 | Store at 4°C, stored under nitrogen |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0874 mL | 10.4371 mL | 20.8742 mL |
| 5 mM | 417.5 μL | 2.0874 mL | 4.1748 mL |
| 10 mM | 208.7 μL | 1.0437 mL | 2.0874 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- Datasheet