EPZ020411 dihydrochloride

製品番号: HY-12970B: Data Sheet 取扱説明書
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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.

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CAS 番号 : 2095432-47-4

容量		在庫状況
MOQ		Minimum order quantity
50 mg		お問い合わせ
100 mg		お問い合わせ
250 mg		お問い合わせ
Other size		お問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other 在庫あり Forms of EPZ020411 dihydrochloride:

EPZ020411 EPZ020411 hydrochloride

Other Forms of EPZ020411 dihydrochloride:

EPZ020411 在庫あり
EPZ020411 hydrochloride 在庫あり

顧客検証

Cell Proliferation/Viability Assay

: EPZ020411 dihydrochloride purchased from MedChemExpress. 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.

Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

PRMT6

0.010 μM (IC₅₀)

体外実験

EPZ020411 dihydrochloride potently inhibits purified PRMT6 enzyme with an IC₅₀ of 0.010 μM, and exhibits over 100-fold selectivity against a variety of other arginine methyltransferases^[1].
EPZ020411(at concentrations greater than 0.01 μM for 48 h) dihydrochloride inhibits PRMT6-mediated H3R2me2a modification in PRMT6-overexpressing A375 cells, with an IC₅₀ of 0.637 ± 0.241 μM^[1].
EPZ020411 (1-1000 μM; 24 h) dihydrochloride reduces the viability of BV2 microglial cells at concentrations of 50, 100 and 1000 μM, while concentrations of 1, 10 and 20 μM do not alter cell viability^[2].
EPZ020411 (2-4 μM; 14 days) dihydrochloride reduces the cell viability of HCT116, HT29, SW480, MC38 and CT26 colorectal cancer (CRC) cell lines, with the maximal effect observed at 4 μM^[3].
EPZ020411 (40 μM) dihydrochloride protects hair cells in postnatal day 2 mouse cochlear explants from cisplatin-induced death and significantly increases hair cell survival rates across all cochlear turns^[4].
EPZ020411 (20-40 μM; 48 h) dihydrochloride potently inhibits the invasive ability of human glioblastoma U87 and LN229 cells in a concentration-dependent manner^[5].

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

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.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	AUC_0-inf	T_max	C_max	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 %

体内実験

EPZ020411 (10 mg/kg; intrathecal injection; 1 h before CCI) dihydrochloride attenuates CCI-induced neuropathic pain, microglial activation, neuroinflammation and glycolysis in the spinal dorsal horn of mice^[2].
EPZ020411 (10 mg/kg; i.p.; once daily; for 3 consecutive weeks) dihydrochloride significantly inhibits the growth of subcutaneous CT26 MSS colorectal cancer xenografts in BALB/c mice^[3].
EPZ020411 (10 mg/kg; i.p.; daily; for 5 consecutive weeks) dihydrochloride slightly reduces the tumor burden of microsatellite-stable colorectal cancer induced by AOM/DSS in C57BL/6 mice^[3].
EPZ020411 (administered via transtympanic route; single dose) dihydrochloride significantly attenuates neomycin-induced chronic hearing loss in 5-day-old C57BL/6 mice and protects the survival of hair cells in the middle and basal turns of the cochlea^[4]
EPZ020411 (10 mg/kg; i.p.; single administration) dihydrochloride significantly attenuates acute hearing loss induced by neomycin combined with furosemide in 28-day-old C57BL/6 mice, maintains hair cell survival, and inhibits cochlear cell apoptosis and reactive oxygen species production^[4].

MedChemExpress (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

分子式

C₂₅H₄₀Cl₂N₄O₃

CAS 番号

2095432-47-4

SMILES

CNCCN(C)CC1=CNN=C1C2=CC=C(C=C2)O[C@H]3C[C@@H](C3)OCCC4CCOCC4.Cl.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

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

[2]. Hua T, et al. PRMT6 deficiency or inhibition alleviates neuropathic pain by decreasing glycolysis and inflammation in microglia. Brain Behav Immun. 2024;118:101-114. [Content Brief]

[3]. Duan J, et al. Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. J Immunother Cancer. 2025;13(3):e010639. Published 2025 Mar 13. [Content Brief]

[4]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020;10(1):133-150. Published 2020 Jan 1. [Content Brief]

[5]. Wang J, et al. PRMT6 facilitates EZH2 protein stability by inhibiting TRAF6-mediated ubiquitination degradation to promote glioblastoma cell invasion and migration. Cell Death Dis. 2024;15(7):524. Published 2024 Jul 23. [Content Brief]