NCB-0846 |
| Catalog No.GC19260 |
NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1792999-26-8
Sample solution is provided at 25 µL, 10mM.
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NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
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 uM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 uM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar[1].
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[1].
References:
[1]. Masuda M, et al. TNIK inhibition abrogates colorectal cancer stemness. Nat Commun. 2016 Aug 26;7:12586.
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