EPZ020411 is a selective inhibitor of PRMT6 with an IC 50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8 . EPZ020411 can be used for the research of cancer
In Vitro
EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells. EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A375 cells Concentration: 0-20 μM Incubation Time: 24 hours Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC 50 of 0.634 μM. Apoptosis AnalysisCell Line: Cultured cochleae cells Concentration: 20-40 μM Incubation Time: 6 hours Result: Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Also reduced hair cell loss caused by cisplatin treatment.
In Vivo
EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model. 1.19 Pharmacokinetic Parameters of EPZ020411 in rats . Rats IV 1 mg/kg Rats SC 5 mg/kg CL (mL/min/kg) 19.7±1.0 V ss (L/kg) 11.1±1.6 t 1/2 (h) 8.54±1.43 9.19±1.60 t max (h) 0.444 C max (ng/mL) 844±306 AUC 0-τ (h·ng/mL) 745±34 2456±135 AUC 0-inf (h·ng/mL) 846±45 2775±181 F (%) 65.6±4.3 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity modelDosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg once Result: Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
IC50& Target:PRMT6 0.01 μM (IC 50 ) PRMT1 0.119 μM (IC 50 ) PRMT8 0.223 μM (IC 50 )
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 分類 | Azoles |
| Subclass | Pyrazoles |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylpyrazoles |
| Alternative Parents | Phenoxy compounds Phenol ethers Aralkylamines Alkyl aryl ethers Oxanes Heteroaromatic compounds Trialkylamines Oxacyclic compounds Dialkylamines Dialkyl ethers Azacyclic compounds Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Phenylpyrazole - Phenoxy compound - Phenol ether - Alkyl aryl ether - Aralkylamine - Monocyclic benzene moiety - Oxane - Benzenoid - Heteroaromatic compound - Tertiary aliphatic amine - Tertiary amine - Dialkyl ether - Secondary aliphatic amine - Ether - Oxacycle - Azacycle - Secondary amine - Organonitrogen compound - Organooxygen compound - Hydrocarbon derivative - Organic oxygen compound - Organic nitrogen compound - Amine - Aromatic heteromonocyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| 分子量 | 442.600 g/mol |
|---|---|
| XLogP3 | 2.700 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 12 |
| Exact Mass | 442.294 Da |
| Monoisotopic Mass | 442.294 Da |
| Topological Polar Surface Area | 71.600 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 519.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
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