Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].
説明 | TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1]. |
In vitro | TNIK-IN-3 (compound 21k) demonstrates inhibitory action against Aurora-A, GCK, and MLK3, with IC50 values of 0.517 μM, 3.657 μM, and 4.552 μM, respectively [1]. Furthermore, it reduces the viability of HCT116 and DLD-1 cells in a dose-dependent manner, presenting IC50s of 4.26 μM and 8.00 μM when applied in concentrations ranging from 0.1 to 100 μM over three days [1]. The compound's effect is also evident in its dose-dependent inhibition of colony formation in these cell types over 10 days with 2.5 to 40 μM concentrations, and in migration suppression with 5 to 20 μM concentrations over 48 hours [1]. Additionally, TNIK-IN-3 dose-dependently decreases the expression of LRP5 and LRP6 proteins and the Wnt target genes AXIN2 and c-Myc in HCT116 cells with 5 to 40 μM concentrations over 48 hours. It significantly diminishes the phosphorylation of JNK1/2 in Hela cells with 5 to 20 μM concentrations over the same duration [1]. |
In vivo | TNIK-IN-3 (compound 21k), administered orally at dosages of 100-150 mg/kg twice daily for 18 days, dose-dependently reduces tumor growth in six-week-old female NOD-SCID mice injected with HCT116 cells[1]. The higher dose of 150 mg/kg resulted in significant tumor suppression without causing weight loss or any noticeable side effects. |
分子量 | 387.41 |
分子式 | C23H18FN3O2 |
CAS No. | 2754265-25-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 75.6 mg/mL (195.1 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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TNIK-IN-3 2754265-25-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin TNIK IN 3 TNIKIN3 Inhibitor inhibitor inhibit