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| Cas No.: | 1792999-26-8 |
| Chemical Name: | NCB0846,NCB 0846 |
| Synonyms: | NCB0846,NCB 0846 |
| SMILES: | C1=CC2N=CNC=2C=C1NC1=NC2=C(O[C@H]3CC[C@@H](O)CC3)C=CC=C2C=N1 |
| Formula: | C21H21N5O2 |
| M.Wt: | 375.17 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM. |
| 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[1]. |
| 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[1]. |
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