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目錄:MedChemExpress LLC>>生化試劑>> NCB-0846 | MCE

NCB-0846 | MCE
  • NCB-0846 | MCE
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更新時間:2023-06-16 17:12:21瀏覽次數(shù):169評價

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CAS 1792999-26-8 純度 99.61%
分子量 375.42 分子式 C??H??N?O?
供貨周期 現(xiàn)貨 規(guī)格 5 mg
貨號 HY-100830 應用領域 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥
NCB-0846 | MCENCB-0846 is an orally available <b>TNIK</b> inhibitor with an <b>IC<sub>50</sub></b> of 21?nM.

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NCB-0846

CAS No. : 1792999-26-8

產(chǎn)品活性:NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21?nM.

研究領域:Stem Cell/Wnt  |  MAPK/ERK Pathway

作用靶點:Wnt  |  MAP4K

In Vitro: NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC50 of 21?nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3?μM and completely inhibits the phosphorylation of TCF4 at a concentration of 3?μM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar.

In Vivo: NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis.

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