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TNIK-IN-3

🥰Excellent
Catalog No. T9556Cas No. 2754265-25-1

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].

TNIK-IN-3

TNIK-IN-3

🥰Excellent
Purity: 99.56%
Catalog No. T9556Cas No. 2754265-25-1
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 SizePriceAvailabilityQuantity
1 mg$108In Stock
5 mg$272In Stock
10 mg$428In Stock
25 mg$687In Stock
50 mg$987In Stock
100 mg$1,530In Stock
1 mL x 10 mM (in DMSO)$298In Stock
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Purity:99.56%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight387.41
FormulaC23H18FN3O2
Cas No.2754265-25-1
SmilesFc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1
Relative Density.1.354 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (129.06 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5812 mL12.9062 mL25.8124 mL129.0622 mL
5 mM0.5162 mL2.5812 mL5.1625 mL25.8124 mL
10 mM0.2581 mL1.2906 mL2.5812 mL12.9062 mL
20 mM0.1291 mL0.6453 mL1.2906 mL6.4531 mL
50 mM0.0516 mL0.2581 mL0.5162 mL2.5812 mL
100 mM0.0258 mL0.1291 mL0.2581 mL1.2906 mL

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