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ILK-IN-2

MCE China：ILK-IN-2

Brand：MedChemExpress (MCE)

Cat. No.HY-18676B

CAS：1333146-24-9

Synonyms：OSU-T315 analog

Purity：98.79%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models.

In Vitro：ILK-IN-2 (0-10 μM, 24 h) shows dose-dependent selective cytotoxicity on CLL-derived cell lines and primary CLL cells, but has minimal impact on normal lymphocytes[1]. ILK-IN-2 (4 μM, 16 h) reduces levels of Mcl-1 and Bcl-xl in CLL cells, triggering caspase activation within those cells[1]. ILK-IN-2 (1-4 μM, 15 min) does not affect proximal membrane signaling of AKT in Mec-1 and OSU-CLL cells[1]. ILK-IN-2 (0-5 μM, 24 h) inhibits the proliferation of prostate and breast cancer cell lines, with IC50 values for LNCaP, PC-3, MDA-MB-231, MDA-MB-468, SKBR3, and MCF-7 being 1.6, 2, 1, 1.5, 1.8, and 2.5 μM respectively, while having no effect on normal epithelial cells[2]. ILK-IN-2 (0-4 μM, 24 h) inhibits PDK2 in PC3 and MDA-MB-231 by suppressing the phosphorylation of Akt at the Ser-473 site[2]. ILK-IN-2 (0-4 μM, 24 h) induces cell death in PC-3 cells through autophagy and apoptosis[2].

In Vivo：ILK-IN-2 (25-50 mg/kg, oral or intraperitoneal injection, once daily, 2-4 weeks) delays leukemia progression in mice and significantly improves the overall survival rate of mice harboring TCL1 leukemia cells[ 1 ]. ILK-IN-2 (25-50 mg/kg, orally, daily, for 35 days) inhibits the growth of PC-3 xenograft tumors in nude mice[2].

IC50 & Target：ILK 0.6 μM (IC50)

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References：

[1]. Ta-Ming Liu, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95.  [Content Brief]

[2]. Su-Lin Lee, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74.  [Content Brief]