Osu03012 NEW
| Price | $31 | $47 | $79 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Osu03012 | CAS No.: 742112-33-0 |
| Purity: 99.22% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Osu03012 |
| Description | Osu03012 (AR-12) is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity. |
| Cell Research | The effect of OSU-03012 on PC-3 cell viability is assessed by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay in six replicates. Cells are grown in 10% FBS- supplemented RPMI 1640 in 96-well, flat-bottomed plates for 24 hours. They are exposed to various concentrations of OSU-03012 (0-10 μM) dissolved in DMSO (final concentration ≤0.1%) in 1% serum-containing RPMI 1640 for different time intervals (~72 hours). Controls receive DMSO vehicle at a concentration equal to that in OSU-03012-treated cells. The medium is removed and replaced by 200 μL of 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide in 10% FBS-containing RPMI 1640. The cells are incubated in the CO2 incubator at 37 °C for 2 hours. Supernatants are removed from the wells, and the reduced 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide dye is solubilized in 200 μL DMSO per well. Absorbance at 570 nm is determined by using a plate reader.(Only for Reference) |
| Kinase Assay | PDK-1 Kinase Assay: This in vitro assay is performed using a PDK-1 kinase assay kit. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or OSU-03012, to activate its downstream serum- and glucocorticoid-regulated kinase which, in turn, phosphorylates the Akt/serum- and glucocorticoid-regulated kinase-specific peptide substrate RPRAATF with [γ-32P]ATP. The 32P-phosphorylated peptide substrate is then separated from the residual [γ-32P]-ATP by using P81 phosphocellulose paper and quantitated in a scintillation counter after three washes with 0.75% phosphoric acid. |
| In vitro | In the MDA-MB-435/LCC6 xenograft model, OSU-03012 significantly reduced the expression of EGFR protein in tumors while also inhibiting the binding of YB-1 to the EGFR promoter. In Huh7 xenografts, OSU-03012 (200 mg/kg) effectively inhibited tumor cell growth. Similarly, oral administration of OSU-03012 in the HMS-97 neurofibroma xenograft model suppressed cell growth. |
| In vivo | At concentrations of 3-5 μM, OSU-03012 can completely inhibit the growth of various tumor cells. In thyroid cancer cells (NPA, WRO, and ARO cells), OSU-03012 acts as an ATP-competitive inhibitor, inhibiting cell proliferation and migration, and inducing apoptosis by suppressing PAK activity and AKT phosphorylation. In hepatocellular carcinoma cell lines (Huh7, Hep3B, and HepG2 cells), OSU-03012 (IC50<1 μM) inhibits cell growth, notably inducing autophagy in Huh7 cells. Additionally, in glioblastoma and PC-3 cells, OSU-03012 promotes apoptosis. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 70 mg/mL (152.03 mM) |
| Keywords | AR12 | AR 12 | Osu03012 |
| Inhibitors Related | MP7 | Rabusertib | M77976 | Polyphyllin I | Sodium dichloroacetate | RS1-PDK1 inhibitor | GSK2334470 | BX795 | Dehydroabiethylamine | Dicoumarol | PS 48 | PHT-427 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Antioxidant Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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