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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].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $65 | In Stock | In Stock | |
| 5 mg | $163 | In Stock | In Stock | |
| 10 mg | $257 | In Stock | In Stock | |
| 25 mg | $412 | In Stock | In Stock | |
| 50 mg | $592 | In Stock | In Stock | |
| 100 mg | $918 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $179 | In Stock | In Stock |
| Description | 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) exhibits inhibitory activity against Aurora-A, GCK, and MLK3 with IC50 values of 0.517 μM, 3.657 μM, and 4.552 μM, respectively [1]. It reduces HCT116 and DLD-1 cell viability dose-dependently, with IC50s of 4.26 μM and 8.00 μM at 0.1 to 100 μM over three days [1]. The compound inhibits colony formation over 10 days (2.5 to 40 μM) and cell migration over 48 hours (5 to 20 μM) [1]. TNIK-IN-3 also dose-dependently decreases LRP5 and LRP6 protein expression, as well as the Wnt target genes AXIN2 and c-Myc in HCT116 cells (5 to 40 μM, 48 hours), and significantly reduces JNK1/2 phosphorylation in Hela cells (5 to 20 μM, 48 hours) [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. |
| Molecular Weight | 387.41 |
| Formula | C23H18FN3O2 |
| Cas No. | 2754265-25-1 |
| Smiles | Fc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1 |
| Relative Density. | 1.354 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (129.06 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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