Contact Us marketing@medicilon.com
Medicilon Logo
|
search icon search icon contact icon menu icon
Medicilon Logo
|
search icon close search icon contact icon menu icon
Message
Contact Us
Close Button
Back To Top
Online Message×
Click switch
Close Button
Customer Center
Customer Center

Researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable

2023-07-11
|
Page View:

54.pngThe methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA.

Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, while its enantiomer UZH1b is essentially inactive. 

The authors thank Medicilon for the synthesis of the UZH1a and UZH1b compounds.

Reference:

Elena V Moroz-Omori, et al. METTL3 Inhibitors for Epitranscriptomic Modulation of Cellular Processes. ChemMedChem. 2021 Oct 6;16(19):3035-3043. doi: 10.1002/cmdc.202100291. 


Return
Relevant News
Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
2023-07-11
Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.
Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
2023-07-11
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
2023-07-11
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).