LDN 209929 2HCl

Modify Date: 2024-02-24 22:55:09

LDN 209929 2HCl Structure
LDN 209929 2HCl structure
Common Name LDN 209929 2HCl
CAS Number 1784281-97-5 Molecular Weight 405.77
Density N/A Boiling Point N/A
Molecular Formula C17H19Cl3N2OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of LDN 209929 2HCl


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].

 Names

Name LDN-209929 dihydrochloride

 LDN 209929 2HCl Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C17H19Cl3N2OS
Molecular Weight 405.77
Storage condition 2-8°C
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