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^[1].

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.

275.35

C₁₃H₉NO₂S₂

C#CC1=CC(/C=C2SC(NC\2=O)=S)=CC=C1OC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yamada N, et al. Correlation between tight binding of inhibitors and their target selectivity toward the non-native state in the DYRK family of kinases. Bioorg Med Chem Lett. 2026;133:130527.  [Content Brief]