RD0448
RD0448 is a potent inhibitor of DYRK1A, DYRK1B, and DYRK2. RD0448 selectively targets the non-native (folded intermediate) state of DYRK1A and DYRK1B. The binding site of RD0448 is hidden in the native state of DYRK1A and DYRK1B, and as a stabilizing binder, it binds tightly to both DYRK1A and DYRK1B, forming a stable complex with slow dissociation kinetics. In contrast, RD0448 targets the native state of DYRK2 without selectivity between its native and non-native states, acting as a weak binder with weaker binding affinity to DYRK2 and forming a rapidly dissociating complex.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C13H9NO2S2
- Masse moléculaire:275.35
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
DYRK1A >64 μM (IC50) |
DYRK1B 52 μM (IC50) |
DYRK2 31 μM (IC50) |
RD0448 (20 s transient heating) selectively targets the non-native conformation of DYRK1A, with its IC50 decreasing from >64 μM to 38 μM under transient heating conditions, and exhibits strong binding to DYRK1A[1].
RD0448 (20-second transient heating treatment) selectively targets the non-natural conformation of DYRK1B, with its IC50 decreasing from 52 μM to 16 μM under transient heating conditions, and it binds tightly to DYRK1B[1].
RD0448 (20 seconds of transient heating at 54°C) did not selectively target the non-native conformation of DYRK2 (transient heating did not enhance inhibitory potency). Its IC50 values are 31 μM and 43 μM under non-heated and transiently heated conditions, respectively, and it does not bind tightly to DYRK2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Masse moléculaire 275.35
-
Formule C13H9NO2S2
-
SMILES
C#CC1=CC(/C=C2SC(NC\2=O)=S)=CC=C1OC
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)