For research use only. Not for therapeutic Use.
LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455)[2].
Haspin: Haploid Germ Cell-Specific Nuclear Protein Kinase, is a serine/threonine kinase expressed in a variety of tissues (e.g., testis, bone marrow, thymus, and spleen). Haspin also plays an important role in mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3) in G2/early prophase, becomes maximal during prometaphase/metaphase and then diminishes during anaphase[1].
DYRKs belong to the CMGC family of ePKs and can be further divided into class 1 kinases DYRK1A and 1B, and class 2 kinases DYRK2, 3, and 4. The activity of DYRKs depends upon autophosphorylation of an essential activation loop tyrosine during synthesis[1].
| Catalog Number | I015388 |
| CAS Number | 1784281-97-5 |
| Synonyms | 3-(2-chloro-7-methoxyacridin-9-yl)sulfanylpropan-1-amine;dihydrochloride |
| Molecular Formula | C17H19Cl3N2OS |
| Purity | ≥95% |
| InChI | InChI=1S/C17H17ClN2OS.2ClH/c1-21-12-4-6-16-14(10-12)17(22-8-2-7-19)13-9-11(18)3-5-15(13)20-16;;/h3-6,9-10H,2,7-8,19H2,1H3;2*1H |
| InChIKey | WOCCOXNODBCCGK-UHFFFAOYSA-N |
| SMILES | COC1=CC2=C(C=C1)N=C3C=CC(=CC3=C2SCCCN)Cl.Cl.Cl |
| Reference | [1]. Gregory D Cuny, et al. Structure-activity Relationship Study of Acridine Analogs as Haspin and DYRK2 Kinase Inhibitors. Bioorg Med Chem Lett [2]. Katrin Kestav, et al. Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin. Curr Med Chem. 2017;24(21):2276-2293. |
