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Chemical Structure| 2070015-25-5 Chemical Structure| 2070015-25-5

Structure of EPZ020411 HCl
CAS No.: 2070015-25-5

Chemical Structure| 2070015-25-5

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EPZ020411 hydrochloride is a selective PRMT6 inhibitor with an IC50 of 10 nM, exhibiting over 10-fold selectivity against PRMT1 and PRMT8. EPZ020411 hydrochloride can be used in cancer research.

Synonyms: EPZ020411 2HCl; EPZ020411 hydrochloride

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Product Details of EPZ020411 HCl

CAS No. :2070015-25-5
Formula : C25H39ClN4O3
M.W : 479.06
SMILES Code : CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2.[H]Cl
Synonyms :
EPZ020411 2HCl; EPZ020411 hydrochloride
MDL No. :MFCD29924736

Safety of EPZ020411 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of EPZ020411 HCl

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEI-OC1 cells 30 μM 24 h To assess the effect of PRMT6 knockdown on cisplatin-induced apoptosis in HEI-OC1 cells. Results showed that PRMT6 knockdown significantly reduced cisplatin-induced apoptosis and ROS accumulation. Theranostics. 2020 Jan 1;10(1):133-150.
Mouse cochlear explants 20 μM and 40 μM 6 h To evaluate the protective effect of EPZ020411 against aminoglycoside- and cisplatin-induced hair cell damage. Results showed that EPZ020411 pretreatment significantly reduced hair cell apoptosis and increased hair cell survival. Theranostics. 2020 Jan 1;10(1):133-150.
GSC23 20 μM 12 h EPZ decreased the levels of RCC1 R214me2 and H3R2me2, reduced the association of RCC1 with chromatin, increased the frequency of mitotic and interphase defects, induced cell cycle arrest (p21 induction), and blocked mitotic progression (p-S10H3 reduction). Mol Cell. 2021 Mar 18;81(6):1276-1291.e9.
GSC576 20 μM 12 h EPZ decreased the levels of RCC1 R214me2 and H3R2me2, reduced the association of RCC1 with chromatin, increased the frequency of mitotic and interphase defects, induced cell cycle arrest (p21 induction), and blocked mitotic progression (p-S10H3 reduction). Mol Cell. 2021 Mar 18;81(6):1276-1291.e9.
CT26 4 µM 4 weeks Long-term EPZ020411 treatment induced an MSI-like phenotype in CT26 cells, with impaired MMR activity. J Immunother Cancer. 2025 Mar 13;13(3):e010639.
SW480 4 µM 24 h To evaluate the effect of EPZ020411 on MMR activity in SW480 cells, results showed that EPZ020411 treatment reduced MMR activity. J Immunother Cancer. 2025 Mar 13;13(3):e010639.
MDA-MB-468 20 µM EPZ020411 inhibits PRMT6 activity, reduces asymmetric dimethylation (ADMA) levels of STAT3, thereby inhibiting Y705 phosphorylation of STAT3. Cell Death Dis. 2023 Oct 9;14(10):655.
MCF-7 20 µM EPZ020411 inhibits PRMT6 activity, reduces asymmetric dimethylation (ADMA) levels of STAT3, thereby inhibiting Y705 phosphorylation of STAT3. Cell Death Dis. 2023 Oct 9;14(10):655.
LN229 cells 20 μM 48 h Inhibited PRMT6 activity, reduced CDC20 and H3R2me2a expression, increased CDKN1B expression, leading to cell cycle arrest at G0/G1 phase Oncogene. 2023 Mar;42(14):1088-1100.
U87 cells 20 μM 48 h Inhibited PRMT6 activity, reduced CDC20 and H3R2me2a expression, increased CDKN1B expression, leading to cell cycle arrest at G0/G1 phase Oncogene. 2023 Mar;42(14):1088-1100.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Aminoglycoside- and cisplatin-induced ototoxicity models Trans-tympanic injection 10 mM Single injection To evaluate the protective effect of EPZ020411 against aminoglycoside- and cisplatin-induced hearing loss in vivo. Results showed that EPZ020411 pretreatment significantly attenuated hearing loss and hair cell damage. Theranostics. 2020 Jan 1;10(1):133-150.
Ncr nu/nu mice GBM brain tumor xenografts Subcutaneous administration 10 mg/kg Daily for three weeks EPZ enhanced the effects of IR in decreasing GSC viability and sphere-forming frequency, markedly reduced RCC1me2 levels, with or without IR. Co-administration of EPZ significantly enhanced the cytotoxic activity of IR, as indicated by significant increases in animal survival. Mol Cell. 2021 Mar 18;81(6):1276-1291.e9.
Mice AOM/DSS-induced CRC model Intraperitoneal injection 10 mg/kg Once daily for 5 weeks To evaluate the therapeutic effect of EPZ020411 on AOM/DSS-induced CRC model, results showed that EPZ020411 treatment reduced the number and size of colon tumors. J Immunother Cancer. 2025 Mar 13;13(3):e010639.
C57BL/6J mice HSV-1-induced PHN model Intrathecal and intraperitoneal 1 μg/5 μl (intrathecal), 10 mg/kg (intraperitoneal) Three consecutive days To evaluate the therapeutic effect of EPZ020411 on HSV-1-induced neuroinflammation and PHN. EPZ020411 reduced neuroinflammation and PHN by enhancing antiviral innate immunity and decreasing HSV-1 load. Brain. 2024 Jul 5;147(7):2552-2565
Female nude mice Breast cancer lung metastasis model Subcutaneous injection 10 mg/kg Daily until the end of the experiment EPZ020411 significantly reduced the number of lung metastasis nodules, extended the overall survival time of mice, and inhibited STAT3 methylation and phosphorylation. Cell Death Dis. 2023 Oct 9;14(10):655.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.44mL

2.09mL

1.04mL

20.87mL

4.17mL

2.09mL

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