Akt1/2 kinase inhibitor Inhibitor
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Akt1/2 kinase inhibitor is an isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, this shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3. The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 muM. Akt is a serine/threonine-specific protein kinase that plays a role in multiple cellular processes such as glucose metabolism, cell proliferation, apoptosis, transcription, and cell migration. Inhibiting Akt1/2 might lead to increased apoptosis and reduced proliferation, as well as changes in processes like wound healing, tumor metastasis, or blood vessel formation. Since the Akt pathway is often hyperactivated in many cancers, targeting Akt1/2 could slow down tumor growth, especially in cancers where these isoforms are prominently involved.
Akt1/2 kinase inhibitor Inhibitor References
- Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. | Barnett, SF., et al. 2005. Biochem J. 385: 399-408. PMID: 15456405
- Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. | Zhao, Z., et al. 2005. Bioorg Med Chem Lett. 15: 905-9. PMID: 15686884
- Apelin induces vascular smooth muscle cells migration via a PI3K/Akt/FoxO3a/MMP-2 pathway. | Wang, C., et al. 2015. Int J Biochem Cell Biol. 69: 173-82. PMID: 26494002
- Metformin Ameliorates Diabetic Cardiomyopathy by Activating the PK2/PKR Pathway. | Yang, Z., et al. 2020. Front Physiol. 11: 425. PMID: 32508669
- [Combination of RNase Binase and AKT1/2 Kinase Inhibitor Blocks Two Alternative Survival Pathways in Kasumi-1 Cells]. | Mitkevich, VA., et al. 2022. Mol Biol (Mosk). 56: 764-773. PMID: 36165015
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Akt1/2 kinase inhibitor, 5 mg | sc-300173 | 5 mg | $243.00 |