LDN-209929 dihydrochloride 是一种有效和选择性的Haspin Kinase抑制剂 (IC50=55 nM)，具有 180 倍的选择性，比 DYRK2 (IC50=9.9 μM)。LDN-209929 是 LDN-192960 的优化物。

LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor ( IC 50 =55 nM) with180-fold selectivity verses DYRK2 ( IC 50 =9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 [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].

1784281-97-5

C17H19Cl3N2OS

405.77

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years