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Akt inhibitors target Akt, also called protein kinase B (PKB), a serine/threonine kinase in cell survival signaling. In 1995 the Akt proto-oncogene product was identified as a target of phosphatidylinositol 3-kinase (PI3K) activated by platelet-derived growth factor. Insulin and insulin-like growth factor 1 activate the kinase through phosphorylation at Thr308 and Ser473. The three isoforms, Akt1, Akt2 and Akt3, phosphorylate substrates that control metabolism, proliferation and apoptosis. The category includes the allosteric inhibitor MK-2206 2HCl, the catalytic-site inhibitor capivasertib and the alkylphospholipid perifosine. SC79, by contrast, promotes Akt phosphorylation and serves as an activator in pathway studies.
CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.
AKTide-2T is a selective substrate for AKT, demonstrating competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. This peptide mimics the optimal phosphorylation sequence of Akt, effectively serving as an inhibitory agent due to the absence of Thr at the S22 position in the wildtype sequence. It is a valuable tool for studying AKT signaling pathways and their implications in various biological processes.
Asperosaponin V is an indirect modulator of key signaling pathways, including PI3K/AKT, BMP-2/p38, and ERK 1/2. This compound stimulates the proliferation of marrow stromal cells and promotes differentiation into osteoblasts, making it valuable for studying bone metabolism. Asperosaponin V holds potential for applications in osteoporosis research and fracture healing studies.
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Anticancer agent 235 is a modulator of the PI3K/AKT/mTOR signaling pathway. It promotes reactive oxygen species (ROS) generation and decreases mitochondrial membrane potential, leading to reduced proliferation of cancer cell lines including HCT116, Caco-2, AGS, and SMMC-772 with IC50 values ranging from 0.35 to 26.9 μM. Furthermore, Anticancer agent 235 effectively induces G2/M cell cycle arrest and apoptosis in HCT116 cells, making it a valuable tool for cancer research applications.
Akt/SKG Substrate Peptide is a synthetic peptide specifically designed as a substrate for Akt/PKB. This peptide is selectively phosphorylated by Akt/PKB and does not undergo phosphorylation by p70S6K or MAPK1, making it an ideal tool for studying the Akt signaling pathway. Its specificity is valuable in research applications focused on cancer, metabolism, and neurological disorders associated with Akt dysregulation.
Crosstide is a peptide analog derived from the glycogen synthase kinase α/β fusion protein sequence, serving as a substrate for Akt. This compound is widely used in research to investigate Akt signaling pathways and assess kinase activity. Crosstide facilitates studies focused on cellular metabolism, growth, and survival, providing valuable insights into the roles of Akt in various biological processes and diseases.
Synonyms: Thyroglobulin from bovine
Thyroglobulin is a 660 kDa dimeric glycoprotein that serves as a substrate in the synthesis of thyroid hormones, thyroxine (T4) and triiodothyronine (T3). Primarily produced by follicular cells of the thyroid, it also functions in the storage of inactive thyroid hormone forms and iodine in the follicular lumen. In research applications, thyroglobulin has been shown to activate Akt kinase activity in FRTL-5 thyroid cells, making it valuable for studies related to thyroid function and signaling pathways.
