Delving into the Latest Updates on MU1250 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CK1δ x CK1ε

Action

inhibitors

Mechanism

CK1δ inhibitors(casein kinase 1 delta inhibitors), CK1ε inhibitors(casein kinase 1 epsilon inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication

Hematologic Neoplasms

Inactive Indication-

Originator Organization

Masaryk University

Active Organization

Masaryk University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC21H17FN6

InChIKeyKINPMBFCIYMYBU-UHFFFAOYSA-N

CAS Registry2377691-79-5

Author: Knapp, Stefan ; Maier, Lukáš ; Bryja, Vítězslav ; Němec, Václav ; Gybel', Tomáš ; Kuster, Bernhard ; Janovská, Pavlína ; Reinecke, Maria ; Berger, Benedict‐Tilman ; Chaikuad, Apirat ; Procházková, Petra ; Kebková, Pavlína ; Khirsariya, Prashant ; Moyano, Paula Martín ; Paruch, Kamil

AbstractCasein kinases 1 (CK1) are key signaling molecules that have emerged recently as attractive therapeutic targets in particular for the treatment of hematological malignancies. Herein, we report the identification of a new class of potent and highly selective inhibitors of CK1α, δ and ϵ. Based on their optimal in vitro and in vivo profiles and their exclusive selectivity, MU1250, MU1500 and MU1742 were selected as quality chemical probes for those CK1 isoforms. At proper concentrations, MU1250 and MU1500 allow for specific targeting of CK1δ or dual inhibition of CK1δ/ϵ in cells. The compound MU1742 also efficiently inhibits CK1α and, to our knowledge, represents the first potent and highly selective inhibitor of this enzyme. In addition, we demonstrate that the central 1H‐pyrrolo[2,3‐b]pyridine‐imidazole pharmacophore can be used as the basis of highly selective inhibitors of other therapeutically relevant protein kinases, e.g. p38α, as exemplified by the compound MU1299.

100 Deals associated with MU1250

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