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3009081-73-3
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Multi-kinase-IN-6
MCE 国际站:Multi-kinase-IN-6
产品活性:Multi-kinase-IN-6 (compound 10e) 是一种多激酶抑制剂,对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 显示出良好的酶抑制活性。Multi-kinase-IN-6 显示出针对 MCF7、HCT116 和 EKVX 的抗增殖活性,IC50 值分别为 3.36 μM、1.40 μM 和 3.49 μM。Multi-kinase-IN-6 在 MCF7 和 HCT116 细胞中显示细胞周期阻滞在 G1/S 期和 G1 期,具有良好的凋亡 (apoptosis) 效果。
研究领域:Neuronal Signaling | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt | Cell Cycle/DNA Damage | Apoptosis
作用靶点:Trk Receptor | Anaplastic lymphoma kinase (ALK) | c-Kit | EGFR | Pim | Casein Kinase | Checkpoint Kinase (Chk) | CDK | Apoptosis
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文献和实验. These residues (Ser 63 and 73) are required to be phosphorylated for efficient transactivation function. The kinases responsible for this modification in vivo are the SAPK/JNKs. These kinases bind with very high affinity to a region in c-Jun termed the delta
, Woodgett JR. (2003) GSK-3: tricks of the trade for a multi-tasking kinase. J Cell Sci. 116 , 1175–1186. 4. Cohen P, Frame S. (2001) The renaissance ofGSK3. Nat Rev Mol Cell Biol. 2 , 769–776. 5. Cohen P, Goedert M. (2004) GSK3 inhibitors
A novel structure-based approach to study the structure and dynamics of flexible multi-domain monomeric protein kinases, which otherwise do not yield diffraction quality crystals, is described. A combination of segmental 15 N-isotopic
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