1784281-97-5

1784281-97-5 structure

Name: LDN 209929 2HCl
Chemical Name: LDN-209929 dihydrochloride
CAS Number: 1784281-97-5
Molecular Formula: C₁₇H₁₉Cl₃N₂OS
Molecular Weight: 405.77
Catalog: Signaling Pathways Cell Cycle/DNA Damage Haspin Kinase
Create Date: 2020-08-07 18:13:54
Modify Date: 2024-02-24 22:55:09
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].

Name	LDN-209929 dihydrochloride

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK Signaling Pathways >> Cell Cycle/DNA Damage >> Haspin Kinase
Target	IC50: 55 nM (haspin kinase) IC50: 9.9 μM (DYRK2)[1]
In Vitro	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].
References	[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.