WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407182
CAS#: 2095432-47-4 (2HCl)
Description: EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 arginine methylation and improves the cytotoxic activity of radiotherapy against GSC brain tumor xenografts.
Hodoodo Cat#: H407182
Name: EPZ020411 HCl
CAS#: 2095432-47-4 (2HCl)
Chemical Formula: C25H40Cl2N4O3
Exact Mass: 442.29
Molecular Weight: 515.520
Elemental Analysis: C, 58.25; H, 7.82; Cl, 13.75; N, 10.87; O, 9.31
Related CAS #: 2095432-47-4 (2HCl) 1700663-41-7 (free base) 2070015-25-5 (HCl)
Synonym: EPZ020411; EPZ-020411; EPZ 020411; EPZ020411 HCl; EPZ020411 hydrochloride
IUPAC/Chemical Name: N1,N2-dimethyl-N1-((3-(4-((1r,3r)-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine dihydrochloride
InChi Key: QCHZLIPYCYHFLI-PZPNUJOOSA-N
InChi Code: InChI=1S/C25H38N4O3.2ClH/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19;;/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28);2*1H/t23-,24-;;
SMILES Code: CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2.[H]Cl.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: RMT6 overexpression has been reported in several cancer types suggesting that inhibition of PRMT6 activity may have therapeutic utility.
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 515.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Huang T, Yang Y, Song X, Wan X, Wu B, Sastry N, Horbinski CM, Zeng C, Tiek D, Goenka A, Liu F, Brennan CW, Kessler JA, Stupp R, Nakano I, Sulman EP, Nishikawa R, James CD, Zhang W, Xu W, Hu B, Cheng SY. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells. Mol Cell. 2021 Mar 18;81(6):1276-1291.e9. doi: 10.1016/j.molcel.2021.01.015. Epub 2021 Feb 3. PMID: 33539787; PMCID: PMC7979509.
2: He Y, Li W, Zheng Z, Zhao L, Li W, Wang Y, Li H. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020 Jan 1;10(1):133-150. doi: 10.7150/thno.37362. PMID: 31903111; PMCID: PMC6929624.
3: Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ, Moradei O, Jin L, Riera T, Porter-Scott M, Moyer MP, Smith JJ, Chesworth R, Copeland RA. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. doi: 10.1021/acsmedchemlett.5b00071. PMID: 26101569; PMCID: PMC4468411.
