ILK-IN-2

SKU: orb1301749

Description

ILK-IN-2 (OSU-T315) is a potent and orally bioavailable small molecule inhibitor of integrin-linked kinase (ILK), exhibiting an IC50 of 0.6 µM. This compound is a valuable research tool for investigating ILK signaling in cancer biology, with utility in both in vitro cellular assays and in vivo xenograft models for studying tumor progression and metastasis.

Research Area

Cell Biology, Metabolism Research, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 1333146-24-9
• MW: 533.59
• Purity: 99.31% (May vary between batches)
• Formula: C₃₀H₃₀F₃N₅O
• SMILES: CNC(=O)CCc1cc(-c2ccc(cc2)-c2ccc(cc2)C(F)(F)F)n(n1)-c1ccc(cc1)N1CCNCC1
• Target: Dehydrogenase,Integrin,Apoptosis,Autophagy,Caspase
• Solubility: DMSO:9 mg/mL (16.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.87 mM)

Bioactivity

• Target IC50:
  ILK:0.6 μM
• In Vivo:
  Athymic nude mice bearing established subcutaneous PC-3 tumors were treated with oral ILK-IN-25 once daily at 25 and 50 mg/kg or vehicle control. The daily administration of ILK-IN-25 at both doses was well tolerated. Treatment with oral ILK-IN-25 in either dose resulted in significant suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively) .
• In Vitro:
  ILK-IN-25 exhibited high in vitro potency against a panel of prostate and breast cancer cell lines (IC(50), 1-2.5 μM), while normal epithelial cells were unaffected. ILK-IN-25 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including glycogen synthase kinase-3β and myosin light chain. Moreover, ILK-IN-25 suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells, which could be rescued by the stable expression of constitutively active ILK . The cytotoxicity of ILK-IN-25 in normal B or T cells was significantly lower (LC50 > 10 μM). ILK-IN-25 had the effect of dose-dependent cytotoxicity toward 2 CLL-derived cell lines, Mec-1 and OSU-CLL (LC50 of 2-3 μM in both) after 24-hour treatment .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Integrin, Inhibitor, OSU-T 315, OSU-T315, OSU-T-315, ILK, ILK IN 2, ILKIN2, ILK-IN-2, inhibit

Compound Identifiers

PubChem CID

51051074