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 (HY-13455) 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 (HY-13455).

Solid

IC50: 55 nM (haspin kinase)
IC50: 9.9 μM (DYRK2)

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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 33.33 mg/mL (82.14 mM; ultrasonic and warming and heat to 60°C)配制储备液