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1233355-57-1

CAS 1233355-57-1
分子式 C17H17ClN2OS
分子量 332.85
MOL 文件 1233355-57-1.mol
1233355-57-1 結(jié)構(gòu)式 1233355-57-1 結(jié)構(gòu)式

常見問題列表

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.

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