LDN-209929,1784281-97-5

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LDN-209929 dihydrochloride

CAS No. : 1784281-97-5

MCE 国际站：LDN-209929 dihydrochloride

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Protein Tyrosine Kinase/RTK

作用靶点：Haspin Kinase  |  DYRK

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.
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.

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