LDN-209929 dihydrochloride

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LDN-209929 dihydrochloride 

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

LDN-209929 dihydrochloride Chemical Structure

CAS No. : 1784281-97-5

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生物活性

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].

IC50 & Target

IC50: 55 nM (haspin kinase)
IC50: 9.9 μM (DYRK2)[1]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

405.77

Formula

C17H19Cl3N2OS
CAS 号

1784281-97-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献

  • [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.

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