1700663-41-7 Usage
Biological Activity
epz020411 is an inhibitor of prmt6.prmt6, a member of the protein arginine methyltransferasefamily, comprises 45 enzymes. the post-translational modifications of prmt6 are important regulators of rna processing, transcriptional regulation, and signal transduction.
in vitro
in biochemical assays, epz020411 was found to be over 100-fold selective for prmt6/8/1 compared to other histone methyltransferases, such as prmt3, prmt4, prmt5 and prmt7. in addition, epz020411 treatment led to a dose-dependent decrease in h3r2 methylation, while treatment with its prmt6-inactive analog did not generate an ic50 at concentrations up to 20 μm [1].
in vivo
animal study found that male sd rats i.v. administered a single dose of epz020411 at 1 mg/kg showed a moderate clearance of 19.7 ml/min/kg, with a volume of distribution at steady state of 11.1 l/kg, and a mean terminal half-life of 8.54 h. following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 was observed, resulting in epz020411 unbound concentration remaining over the prmt6 ic50 for more than 12 h [1].
IC 50
10 nm
references
[1] mitchell lh, et al. aryl pyrazoles as potent inhibitors of arginine methyltransferases: identification of the first prmt6 toolcompound. acs med chem lett. 2015 apr 6;6(6):655-659.
Check Digit Verification of cas no
The CAS Registry Mumber 1700663-41-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,7,0,0,6,6 and 3 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1700663-41:
(9*1)+(8*7)+(7*0)+(6*0)+(5*6)+(4*6)+(3*3)+(2*4)+(1*1)=137
137 % 10 = 7
So 1700663-41-7 is a valid CAS Registry Number.
1700663-41-7Relevant articles and documents
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound
Mitchell, Lorna H.,Drew, Allison E.,Ribich, Scott A.,Rioux, Nathalie,Swinger, Kerren K.,Jacques, Suzanne L.,Lingaraj, Trupti,Boriack-Sjodin, P. Ann,Waters, Nigel J.,Wigle, Tim J.,Moradei, Oscar,Jin, Lei,Riera, Tom,Porter-Scott, Margaret,Moyer, Mikel P.,Smith, Jesse J.,Chesworth, Richard,Copeland, Robert A.
, p. 655 - 659 (2015)
A novel aryl pyrazole series of arginine methyltransferase inhibitors has been identified. Synthesis of analogues within this series yielded the first potent, selective, small molecule PRMT6 inhibitor tool compound, EPZ020411. PRMT6 overexpression has bee
