LDN-192960 HCl
Haspin and DYRK2/3 inhibitor / LDN-192960 is a potent inhibitor of Haspin (IC50 = 10 nM), DYRK2 (IC50 = 2 nM), and DYRK3 (IC50 = 19 nM).1,2 It induced cytotoxicity and growth inhibition in multiple myeloma and triple negative breast cancer cells and triple negative breast cancer mouse allo/xenografts via partial inhibition of 26S proteasome activity.3
Biochemicals & reagents
184582-62-5
1) Patnaik et al. (2008), Identification of Small Molecules Inhibitors of the Mitotic Kinase Haspin by High Throughput Screening using a Homogenous Time-Resolved Fluorescence Resonance Transfer Assay; J. Biomol. Screen., 13 1025 2) Cuny et al. (2010), Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase3 inhibitors; Bioorg. Med. Chem. Lett., 20 3491 3) Banerjee et al. (2019), Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression; Proc. Natl. Acad. Sci. USA, 116 24881
-20°C
TARGET: Kinase -- PATHWAY: Cell cycle -- RESEARCH AREA: Ubiquitin/Proteasome -- DISEASE AREA: Cancer