TNIK-IN-3

SKU: orb1685277

Description

TNIK-IN-3 is a potent, orally bioavailable, and selective TNIK kinase inhibitor (IC50=0.026 µM) with additional activity against Flt4, Flt1, and DRAK1. It is a valuable research tool for studying TNIK's role in pathways relevant to colorectal cancer, supporting both in vitro and in vivo experimental models.

Research Area

Cell Biology, Neuroscience, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2754265-25-1
• MW: 387.41
• Purity: 99.56% (May vary between batches)
• Formula: C₂₃H₁₈FN₃O₂
• SMILES: Fc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1
• Target: DAPK,Wnt/beta-catenin
• Solubility: DMSO:50 mg/mL (129.06 mM)

Bioactivity

• 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. The higher dose of 150 mg/kg resulted in significant tumor suppression without causing weight loss or any noticeable side effects.
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• 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 . 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 . The compound inhibits colony formation over 10 days (2.5 to 40 μM) and cell migration over 48 hours (5 to 20 μM) . 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) .
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Storage & Handling

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

Alternative Names

betacatenin, beta-catenin, bcatenin, βcatenin, TNIK IN 3, TNIK, TNIKIN3, TNIK-IN-3, Wnt/β-catenin, Wnt, Wnt/betacatenin, Wnt/b-catenin

Compound Identifiers

PubChem CID

162641720