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Submit ReviewAkti-1/2 is a potent and selective dual Akt1 and 2 inhibitor (IC50 values are 50 and 210 nM, respectively). Selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. Sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Also enhances CAR and TCR retroviral transduction of human T cells. Active in vivo.
分子量 | 551.64 |
公式 | C34H29N7O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 612847-09-3 |
PubChem ID | 10196499 |
InChI Key | BIWGYFZAEWGBAL-UHFFFAOYSA-N |
Smiles | O=C1NC2=C(C=CC=C2)N1C(CC3)CCN3CC(C=C4)=CC=C4C5=NC6=CC(N=CN7)=C7C=C6N=C5C8=CC=CC=C8 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 11.03 | 20 温和加热 |
以下数据基于产品分子量 551.64。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 9.06 mL | 45.32 mL | 90.64 mL |
1 mM | 1.81 mL | 9.06 mL | 18.13 mL |
2 mM | 0.91 mL | 4.53 mL | 9.06 mL |
10 mM | 0.18 mL | 0.91 mL | 1.81 mL |
参考文献是支持产品生物活性的出版物。
DeFeo-Jones D et al (2005) Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol.Cancer Ther. 4 271 PMID: 15713898
Barnett et al (2005) Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem. J. 385 399 PMID: 15456405
Lindsley et al (2005) Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg.Med.Chem.Lett. 15 761 PMID: 15664853
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214
Klebanoff et al (2017) Inhibition of AKT signaling uncouples T cell differentiation from expansion for receptor-engineered adoptive immunotherapy. JCI Insight 2 e95103 PMID: 29212954
If you know of a relevant reference for Akti-1/2, please let us know.
关键词: Akti-1/2, Akti-1/2 supplier, Akt1/2, inhibitors, inhibits, potent, selective, PKB, protein, kinase, B, sensitizes, apoptosis, viral, transduction, enhancer, enhances, Akt, Inhibitor, VIII, (Protein, Kinase, B), Protein, B/Akt, Viral, Transduction, Enhancers, 5773, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Akti-1/2 的部分引用包括:
Viviana I et al (2019) Wnt-induced activation of glucose metabolism mediates the in vivo neuroprotective roles of Wnt signaling in Alzheimer disease. J Neurochem 149 54-72 PMID: 30300917
Claudio et al (2022) PD-1-induced T cell exhaustion is controlled by a Drp1-dependent mechanism. Mol Oncol 16 188-205 PMID: 34535949
Aurélie et al (2022) Exosomes from EGFR-Mutated Adenocarcinoma Induce a Hybrid EMT and MMP9-Dependant Tumor Invasion. Cancers (Basel) 14 PMID: 35954442
Lucie et al (2022) Regulation of Stress-Activated Kinases in Response to Tacaribe Virus Infection and Its Implications for Viral Replication. Viruses 14 PMID: 36146824
Adriano et al (2022) TSC22D4 interacts with Akt1 to regulate glucose metabolism. Sci Adv 8 eabo5555 PMID: 36269831
Margitta et al (2022) Pannexin-1 Activation by Phosphorylation Is Crucial for Platelet Aggregation and Thrombus Formation. Int J Mol Sci 23 PMID: 35563450
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Kodaka et al (2020) Characterization of a novel compound that promotes myogenesis via Akt and transcriptional co-activator with PDZ-binding motif (TAZ) in mouse C2C12 cells. PLoS One 15 e0231265 PMID: 32267872
Zhong et al (2018) Tyro3 is a podocyte protective factor in glomerular disease. JCI Insight 3 PMID: 30429374
Anna M et al (2021) Gαq activation modulates autophagy by promoting mTORC1 signaling. Nat Commun 12 4540 PMID: 34315875
Charles G et al (2021) EGFR Activates a TAZ-Driven Oncogenic Program in Glioblastoma. Cancer Res 81 3580-3592 PMID: 33910930
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Human osteosarcoma cells were incubated with 10 μM Akti-1/2 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. Akti-1/2 abolished LPA-induced COX-2 expression.
MG-63 cells were incubated with PD169316 (25 μM), LY294002 (10 μM) or Akt-1/2 (5 μM Akt-I) for 30 min prior to 15d-PGJ2 treatment (20 μM) for 1 h to follow pAkt expression using Western blot. Akt-1/2 completely blocked 15d-PGJ2-induced Akt phosphorylation in MG-63 cells.