2. Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Histone Methyltransferase Reactive Oxygen Species (ROS) Apoptosis
  4. EPZ020411 dihydrochloride

EPZ020411 dihydrochloride 是一种选择性、可透过血脑屏障 PRMT6 抑制剂，其 IC50 为 0.010 μM。\nEPZ020411 dihydrochloride 可阻断 PRMT6 介导的组蛋白 H3R2 甲基化，并减少 ROS 的生成、抑制凋亡 (Apoptosis)。EPZ020411 dihydrochloride 可用于神经性疼痛、结直肠癌、耳毒性、听力损失及胶质母细胞瘤的相关研究。

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CAS No. : 2095432-47-4

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EPZ020411 dihydrochloride 相关抗体

Top Publications Citing Use of Products

    EPZ020411 dihydrochloride purchased from MCE. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413.  [Abstract]

    EPZ020411(PRMT6i; 200-1000 nM) in combination with GSK591(PRMT5i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

    查看 Histone Methyltransferase 亚型特异性产品:

    查看所有亚型
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma[1][2][3][4][5].

    IC50 & Target[1]

    PRMT6

    0.010 μM (IC50)

    体外研究
    (In Vitro)

    EPZ020411 dihydrochloride 可强效抑制纯化的 PRMT6 酶，其 IC50 为 0.010 μM，且对多种其他精氨酸甲基转移酶的选择性超过 100 倍[1]。
    EPZ020411 (大于 0.01 μM; 48 h) dihydrochloride 可在过表达 PRMT6 的 A375 细胞中抑制 PRMT6 介导的 H3R2me2a 修饰，其 IC50 为 0.637 ± 0.241 μM[1]。
    EPZ020411 (1-1000 μM; 24 h) dihydrochloride 可在 50、100 和 1000 μM 浓度下降低 BV2 小胶质细胞的活力，而 1、10 和 20 μM 浓度则不会改变细胞活力[2]。
    EPZ020411 (2-4 μM；14 天) dihydrochloride 可降低 HCT116、HT29、SW480、MC38 和 CT26 结直肠癌 (CRC) 细胞系的细胞存活率，在 4 μM 时观察到最大效应[3]。
    EPZ020411 (40 μM) dihydrochloride 可保护出生后第 2 天小鼠耳蜗外植体毛细胞免受顺铂诱导的死亡，显著提高所有耳蜗回的毛细胞存活率[4]。
    EPZ020411 (20-40 μM; 48 h) dihydrochloride 可浓度依赖性地强效抑制人胶质母细胞瘤 U87 和 LN229 细胞的侵袭能力[5]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    EPZ020411 dihydrochloride 相关抗体:

    Western Blot Analysis[3]

    Cell Line: SW480 human CRC cells
    Concentration: 2, 4 μM (48 h incubation)
    Incubation Time: 48 h
    Result: Stimulated phosphorylation of STAT1 and IRF3 in SW480 cells.

    Cell Invasion Assay[5]

    Cell Line: human glioblastoma U87, human glioblastoma LN229
    Concentration: 20 μM, 40 μM
    Incubation Time: 48 h (pretreatment prior to assay)
    Result: Reduced invasive cell numbers in U87 and LN229 cells at 20 μM.
    Further reduced invasive cell numbers in both cell lines at 40 μM, with statistical significance relative to untreated cells (****p < 0.0001 for U87; ***p < 0.001 for LN229).

    Western Blot Analysis[5]

    Cell Line: human glioblastoma U87, human glioblastoma LN229
    Concentration: 20 μM, 40 μM
    Incubation Time: 48 h
    Result: Reduced global H3R2me2a levels in both U87 and LN229 cells relative to untreated cells.
    Increased TRAF6 protein expression in both U87 and LN229 cells relative to untreated cells.
    药代动力学
    (Parmacokinetics)
    Species Dose Route CL Vss T1/2 AUC0-inf Tmax Cmax Bioavailability
    Rat[1] 1 mg/kg i.v. 19.7 ± 1.0 mL/min/kg 11.1 ± 1.6 L/kg 8.54 ± 1.43 h 846 ± 45 ng·h/mL / / /
    Rat[1] 5 mg/kg s.c. / / 9.19 ± 1.60 h 2775 ± 181 ng·h/mL 0.444 h 844 ± 306 ng/mL 65.6 ± 4.3 %
    体内研究
    (In Vivo)

    EPZ020411 (10 mg/kg；鞘内注射；CCI 前 1 h) dihydrochloride 可减轻小鼠脊髓背角中 CCI 诱导的神经病理性疼痛、小胶质细胞活化、神经炎症及糖酵解[2]。
    EPZ020411 (10 mg/kg；腹腔注射；每日一次；持续 3 周) dihydrochloride 可显著抑制 BALB/c 小鼠皮下接种的 CT26 MSS 结直肠癌异种移植物的生长[3]。
    EPZ020411 (10 mg/kg；腹腔注射；每日；连续 5 周) dihydrochloride 可轻度降低 AOM/DSS 诱导的 C57BL/6 小鼠微卫星稳定型结直肠癌的肿瘤负荷[3]。
    EPZ020411 (经鼓膜给予；单次) dihydrochloride 可显著减轻 5 日龄 C57BL/6 小鼠中新霉素诱导的慢性听力损失，并保护耳蜗中回和基回的毛细胞存活[4]
    EPZ020411 (10 mg/kg；腹腔注射；单次) dihydrochloride 可显著减轻新生 28 天 C57BL/6 小鼠由新霉素联合呋塞米诱导的急性听力损失，维持毛细胞存活，并抑制耳蜗细胞凋亡及活性氧生成[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57BL/6 (5 days old, neomycin-induced chronic ototoxicity model)[4]
    Dosage: 10 mM (1 μl)
    Administration: trans-tympanic; single dose
    Result: Showed significantly reduced ABR and DPOAE threshold elevation at all tested frequencies (4, 8, 16, 24, 32 kHz) compared to saline-pretreated ears.
    Increased myosin 7a-positive hair cell survival significantly in the middle and basal cochlear turns relative to neomycin-only controls.
    Animal Model: C57BL/6 (postnatal day 28, cisplatin-induced ototoxicity model)[4]
    Dosage: 10 mM (5 μl)
    Administration: trans-tympanic; single dose
    Result: Showed significantly reduced ABR and DPOAE threshold elevation at all tested frequencies (4, 8, 16, 24, 32 kHz) at days 4, 7, and 14 post-cisplatin compared to saline-pretreated ears.
    Increased myosin 7a-positive hair cell survival significantly in the middle and basal cochlear turns relative to cisplatin-only controls.
    Reduced caspase 3/7-positive cells in the middle turn from 22.01 ± 4.435 to 4.018 ± 3.684 per 200 μm.
    Reduced MitoSox-Red-positive cells in the middle turn from 43.62 ± 6.740 to 0.9616 ± 0.9760 per 200 μm.
    分子量

    515.52

    Formula

    C25H40Cl2N4O3
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    EPZ020411 dihydrochloride 相关分类

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    • Do most proteins show cross-species activity?

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    Keywords:

    EPZ0204112095432-47-4EPZ 020411EPZ-020411Histone MethyltransferaseReactive Oxygen Species (ROS)ApoptosisBV2 microglial cellsU87 cellscGAS-STING signalingPRMT6HIF-1αA375 cellsHCT116 cellshistone H3R2glioblastomaLN229 cellsInhibitorinhibitorinhibit

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