akt i 1

AKT-I-1 is a selective and reversible inhibitor of Akt1.

Akt-I-1,2 is a selective inhibitor of Akt1 and Akt2.

AKT inhibitor VIII (AKTi-1/2) is a highly specific inhibitor of Akt1/2, with IC50 values of 58 nM and 210 nM respectively, demonstrating approximately 36-fold greater selectivity for Akt1 over Akt3.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

(±)-Evodiamine is an alkaloid isolated from Evodiae fructus and a topoisomerase I inhibitor. It also inhibits adipocyte differentiation and diabetes by downregulating IGF-1/HIF-1α and IL-6/STAT pathways. As an inhibitor of NF-κB activation, it suppresses invasion, promotes apoptosis, and inhibits TNF-induced Akt activation.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks (Kis of 4 nM, 6 nM, 2 nM, and 1 nM for PI3Kα, β, δ, and γ, respectively), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

DHW-221 is an orally active dual PI3K/mTOR inhibitor demonstrating potent inhibition at nanomolar levels across all four Class I PI3K isoforms and mTOR (PI3Kα, IC50= 0.50 nM; PI3Kβ, IC50= 1.9 nM; PI3Kγ, IC50= 1.8 nM; PI3Kδ, IC50= 0.74 nM; mTOR, IC50= 3.9 nM). By blocking the PI3K/Akt/mTOR pathway, DHW-221 induces mitochondrial apoptosis and paraptosis (through endoplasmic reticulum stress and MAPK signaling) and causes cell cycle arrest, thereby inhibiting cell migration, invasion, and angiogenesis to exert its antitumor effects. It suppresses tumor growth in A549/Taxol and HCC827 mouse models and is applicable in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer[1][2][3].

Anti-DCBLD2/ESDN Antibody (FA19-1) is a humanized monoclonal antibody targeting Discoidin, CUB and LCCL domain-containing protein 2 (DCBLD2/ESDN/CLCP1). DCBLD2 is a type I transmembrane protein overexpressed in various malignancies (e.g., lung adenocarcinoma, glioma) and acts as a signal relay for growth factor signaling like EGFR. FA19-1 specifically binds to the extracellular domain of DCBLD2, blocking its mediated signaling—such as AKT activation or cisplatin-induced EMT—thereby inhibiting tumor cell migration, invasion, and distant metastasis.

Anti-IGF1R/CD221 Antibody is a highly specific monoclonal antibody targeting the Type I Insulin-like Growth Factor Receptor (IGF-1R/CD221). By binding to the extracellular domain of IGF-1R, this antibody effectively blocks the interaction with its ligands IGF-1 and IGF-2, thereby inhibiting the activation of downstream PI3K/Akt and MAPK signaling pathways. It is a vital tool for researching tumor cell growth inhibition, apoptosis induction, and transmembrane signaling mechanisms.

1. Artemitin (Erianthin) has anti-inflammatory activity. 2. Artemitin (Erianthin) protects endothelial function by acting as antioxidant and antiapoptotic agent and through the activation of ERK1/2 and Akt. 3. Intravenous injection of Artemitin (Erianthin)(.75 mg/kg) significantly reduces the hypertensive response to angiotensin I while increases the average length of bradykinin-induced hypotension.

Oldenlandoside I ((E)-6-O-p-coumaroyl scandoside methyl ester) is a natural product isolated from Hedyotis diffusa exhibiting potential antiproliferative activity. It induces apoptosis in SKM-1 cells in combination with p-coumaric acid, associated with caspase activation and inhibition of PI3K/Akt pathway proteins.

Eutypenes I (Compound 9) inhibits the secretion of VEGF-A, hampers the activation of VEGFR, and disrupts its downstream Erk/Akt signaling pathway. It also suppresses the migration of HMEC-1 cells and demonstrates anti-angiogenic activity in a Sprague-Dawley rat model.