1233355-57-1
1233355-57-1 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
生物活性
LDN-209929 dihydrochloride 是一種有效和選擇性的 haspin kinase 抑制劑 (IC50=55 nM),具有 180 倍的選擇性,比 DYRK2 (IC50=9.9 μM)。LDN-209929 是 LDN-192960 (HY-13455) 的優(yōu)化物。靶點(diǎn)
IC50: 55 nM (haspin kinase)IC50: 9.9 μM (DYRK2)
體外研究
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.