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OSU-03012 is a novel and potent inhibitor of PDK-1. OSU-03012 exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase (PI3K)/Akt pathway. It has an IC50 of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1 (PDK-1), and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM. OSU-03012 induces apoptosis of chronic lymphocytic leukemia (CLL) cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways. A recent study shows that OSU-03012 could enhance the susceptibility of (Bcr)-Abl mutant cell lines to imatinib-induced apoptosis. OSU-03012 may lead to cell swelling and shortening of AP via reduced ATP production in mouse ventricular cells.
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Source | Mol Med Rep (2015). Figure 2.OSU‑03012 |
| Method | Apoptosis detection | |
| Cell Lines | LX2 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 or 72 h | |
| Results | Aapoptosis was not induced in LX2 cells treated with OSU‑03012, compared with those treated with DMSO. These results indicated that OSU‑03012 did not inhibit the growth of LX2 cells via the induction of apoptosis. |
| Cell Experiment | |
|---|---|
| Cell lines | VS and HMS-97 cells |
| Preparation method | Cell proliferation assay VS and HMS-97 cells were grown in polylysine/laminin-coated 96-well plates (5 × 103 to 1 × 104 per well). After incubation at 37°C for 24 hrs, cells were treated with various concentrations of OSU-03012 or DMSO as a vehicle control at 37°C for another 48 hrs. To assess cell proliferation, the CellTiter 96®AQueous One Solution Cell Proliferation Assay (Promega) was used according to the manufacturer’s instructions. Briefly, 20μl of CellTiter 96® AQueous One Solution Reagent were added to each well and incubated at 37°C for 1 to 4 hrs. The amount of colored formazan produced in the cells was measured at 490nm using a Victor3 1420 Multilabel Counter (Perkin Elmer). The percentage of cell proliferation was plotted against the concentrations of OSU-03012, and the IC50 (defined as the drug concentration at which the population of viable cells was reduced by 50%) was determined using CalcuSyn software (Biosoft). The experiments were replicated six times, and the mean IC50 was calculated. |
| Concentrations | 0~16µM |
| Incubation time | 48h |
| Animal Experiment | |
|---|---|
| Animal models | Schwannoma xenografts in severe combined immunodeficiency mice (SCID) |
| Formulation | methylcellulose (0.5%, w/v) and Tween 80 (0.1%, w/v) in sterile water |
| Dosages | 200 mg/kg/day |
| Administration | oral gavage |
| Molecular Weight | 460.45 |
| Formula | C26H19F3N4O |
| CAS Number | 742112-33-0 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDK1 Products |
|---|
| MP7
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor. |
| PDKtide
PDKtide is a biological active peptide. |
| PDK1-IN-RS2
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1. |
| PS47
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48. |
| PS210
PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
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