TNIK-IN-3

SKU: orb2900255

Description

TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.

Research Area

Neuroscience

Key Properties

• CAS Number: 2754265-25-1
• MW: 387.41
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₈FN₃O₂
• SMILES: Fc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1
• Target: Wnt/beta/catenin
• Solubility: In Vitro: DMSO : 83.33 mg/mL (215.10 mM; Ultrasonic )

Bioactivity

• In Vivo:
  TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner. Animal model: Six-week-old female NOD-SCID mice were injected with HCT116 cells. Dosage: 100, 150 mg/kg. Administration: p.o. twice daily for 18 days. Result: Significantly inhibited tumor growth at a dose of 150 mg/kg.
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• In Vitro:
  TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively. TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively. TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells. TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells. TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells. TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells. Cell Viability Assay Cell line: HCT116 and DLD-1 cells. Concentration: 0.1-100 μM Incubation time: 3 days. Result: Inhibited cell viability in a dose-dependent manner. Cell Viability Assay Cell line: HCT116 cells. Concentration: 5, 10, 20, 40 μM. Incubation time: 48 hours. Result: Inhibited the expression of Wnt target genes AXIN2 and c-Myc, LRP5 and LRP6 proteins.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Wnt/beta/catenin