Molecular structure of OSU 03012, CAS Number: 742112-33-0
OSU 03012 (CAS 742112-33-0)
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Alternate Names:
AR-12; OSU-03012
Application:
OSU 03012 is a PDK1 inhibitor and inducer of caspase and p53-independent apoptosis
CAS Number:
742112-33-0
Purity:
≥98%
Molecular Weight:
460.45
Molecular Formula:
C26H19F3N4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
OSU 03012 is a potent inhibitor of PDK1 (IC50 = 5 muM). It causes a dose-dependent induction of cell death regardless of the presence or absence of mutated p53. Studies have shown that upon treatment of cells with OSU 03012 there is an accumulation of reactive oxygen species (ROS) in the cell, which may contribute to cell death through oxidative damage. Exposure to ionizing radiation following treatment with OSU 03012 causes an increase in cell death, which is also caspase-independent.
OSU 03012 (CAS 742112-33-0) References
- A novel celecoxib derivative, OSU03012, induces cytotoxicity in primary CLL cells and transformed B-cell lymphoma cell line via a caspase- and Bcl-2-independent mechanism. | Johnson, AJ., et al. 2005. Blood. 105: 2504-9. PMID: 15454489
- OSU-03012 promotes caspase-independent but PERK-, cathepsin B-, BID-, and AIF-dependent killing of transformed cells. | Yacoub, A., et al. 2006. Mol Pharmacol. 70: 589-603. PMID: 16622074
- Chemopreventive and bioenergetic signaling effects of PDK1/Akt pathway inhibition in a transgenic mouse model of prostate cancer. | Sargeant, AM., et al. 2007. Toxicol Pathol. 35: 549-61. PMID: 17562488
- Cyclooxygenase-2 independent effects of cyclooxygenase-2 inhibitors on oxidative stress and intracellular glutathione content in normal and malignant human B-cells. | Ryan, EP., et al. 2008. Cancer Immunol Immunother. 57: 347-58. PMID: 17668203
- OSU-03012, a novel celecoxib derivative, is cytotoxic to myeloma cells and acts through multiple mechanisms. | Zhang, S., et al. 2007. Clin Cancer Res. 13: 4750-8. PMID: 17699852
- Sensitivity to the non-COX inhibiting celecoxib derivative, OSU03012, is p21(WAF1/CIP1) dependent. | Ding, H., et al. 2008. Int J Cancer. 123: 2931-8. PMID: 18798266
- OSU-03012, a novel celecoxib derivative, induces reactive oxygen species-related autophagy in hepatocellular carcinoma. | Gao, M., et al. 2008. Cancer Res. 68: 9348-57. PMID: 19010909
- OSU-03012 sensitizes TIB-196 myeloma cells to imatinib mesylate via AMP-activated protein kinase and STAT3 pathways. | Bai, LY., et al. 2010. Leuk Res. 34: 816-20. PMID: 20006997
- OSU-03012, a novel celecoxib derivative, induces cell swelling and shortens action potential duration in mouse ventricular cells. | Yamamoto, S., et al. 2010. Biomed Res. 31: 413-7. PMID: 21187652
- Effects of small molecule inhibitors of PI3K/Akt/mTOR signaling on neuroblastoma growth in vitro and in vivo. | Segerström, L., et al. 2011. Int J Cancer. 129: 2958-65. PMID: 21717457
- OSU-03012 suppresses GRP78/BiP expression that causes PERK-dependent increases in tumor cell killing. | Booth, L., et al. 2012. Cancer Biol Ther. 13: 224-36. PMID: 22354011
- Design and Function of Engineered Protein Nanocages as a Drug Delivery System for Targeting Pancreatic Cancer Cells via Neuropilin-1. | Murata, M., et al. 2015. Mol Pharm. 12: 1422-30. PMID: 25811429
- Acupuncture Administration Improves Cognitive Functions and Alleviates Inflammation and Nuclear Damage by Regulating Phosphatidylinositol 3 Kinase (PI3K)/Phosphoinositol-Dependent Kinase 1 (PDK1)/Novel Protein Kinase C (nPKC)/Rac 1 Signaling Pathway in Senescence-Accelerated Prone 8 (SAM-P8) Mice. | Li, G., et al. 2019. Med Sci Monit. 25: 4082-4093. PMID: 31152645
- OSU-03012 Disrupts Akt Signaling and Prevents Endometrial Carcinoma Progression in vitro and in vivo. | Ding, L., et al. 2021. Drug Des Devel Ther. 15: 1797-1810. PMID: 33958857
- Celecoxib Analogues for Cancer Treatment: An Update on OSU-03012 and 2,5-Dimethyl-Celecoxib. | Sobolewski, C. and Legrand, N. 2021. Biomolecules. 11: PMID: 34356673
Inhibitor of:
APPL2, FRBZ1, PDK1, PIPK II α, PKC λ/ι, and TFE3.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
OSU 03012, 5 mg | sc-364560 | 5 mg | $109.00 | |||
OSU 03012, 25 mg | sc-364560A | 25 mg | $349.00 |