akt-in-2

AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1).

VEGFR-2/AKT-IN-2 (Compound 5) is an inhibitor of VEGFR-2/AKT, with an IC50 of 0.061 μM for VEGFR in human liver cancer cells. It reduces total and phosphorylated AKT in cells, increases BAX and caspase-3 levels, and decreases Bcl-2, thereby inducing apoptosis. Additionally, VEGFR-2/AKT-IN-2 halts the cell cycle at the S phase and inhibits the growth of human liver cancer cells.

PI3K/AKT-IN-2, a dual inhibitor of PI3K and AKT, prevents the epithelial-mesenchymal transition (EMT) and promotes apoptosis. Additionally, it impedes tubulin polymerization.

AKT-IN-25 (Compound 14a) is an inhibitor of Akt that prevents the phosphorylation of Akt, thereby hindering the PI3K/Akt/mTOR signaling pathway. It arrests the cell cycle at the G1 phase, inhibits the migration of PANC-1 cells, and suppresses the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2, with IC50 values of 3.05, 1.32, and 3.85 μM, respectively.

AKT-IN-24 (Compound M17) is an allosteric inhibitor of AKT exhibiting antitumor activity. In combination with Trametinib, it targets the AKT/mTOR and MEK/ERK signaling pathways while inhibiting epithelial-mesenchymal transition, resulting in a synergistic suppression effect on TNBC. This combination promotes apoptosis and inhibits cell proliferation and migration.

AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin Homology (PH) domain of AKT. It is useful for research related to cell proliferation and cancer involving the AKT pathway.

AKT-IN-27 (4a) is a potential anticancer drug that functions by selectively targeting Akt-driven signaling pathways. It induces apoptosis by activating caspase-3, causing G2/M phase cell cycle arrest, and disrupting mitochondrial membrane potential. AKT-IN-27 (4a) is applicable in research on triple-negative breast cancer (TNBC).

AKT-IN-21 (compound C36) is a potent AKT inhibitor with broad-spectrum cytotoxic and anticancer properties. It induces apoptosis in cancer cells by blocking the cell cycle and downregulating the PI3K/AKT pathway.

AKT-IN-28 is an allosteric inhibitor of Akt and a derivative of Shikonin. It effectively binds to Akt's allosteric site through hydrophobic and hydrogen bond interactions, with a Kd value of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, inducing apoptosis in KRAS-mutant colorectal cancer cells, arresting the cell cycle at the G2/M phase, and suppressing cell proliferation, migration, and metabolism.

AKT-IN-22 (compound 0R4) serves as a potent allosteric inhibitor of AKT, exhibiting anticancer properties [1].

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.

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2. 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.

PI3K/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

ZINC00640089 is a selective lipid carrier protein-2 (LCN2) inhibitor. ZINC00640089 inhibited cell proliferation and cell viability, and reduced AKT phosphorylation in SUM149 cells. ZINC00640089 can be used to study inflammatory breast cancer (IBC).

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2/Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT/Nrf-2/HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

ZINC00784494 is a selective inhibitor of LCN2 (lipocalin-2), which inhibits cancer cell proliferation and reduces AKT phosphorylation levels, prevents the transition of the cell cycle from the G0/G1 phase to the S phase, and promotes apoptosis. It can be used for the study of inflammatory breast cancer (IBC).

ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate is a synthetic compound belonging to the curcumin family. It is involved in the regulation of immune response and inflammation through inhibition of the NF-κB signaling pathway, in the regulation of antioxidant response through activation of the Nrf2 signaling pathway, and in the regulation of cell survival and proliferation through inhibition of the Akt signaling pathway.

CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

Carpaine is a natural product exhibiting antimalarial activity, with an approximate IC50 of 4μM against P. falciparum in NL20 cells. It demonstrates cardioprotective and anti-inflammatory effects by activating FAK, ERK1/2, and AKT pathways while inhibiting ROS production.

NSC117079 is a novel PHLPP1/2 (Pleckstrin homology domain and leucine rich repeat protein phosphatase) inhibitor that activates neuronal AKT and ameliorates staurosporine-induced cell death in neurons.

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).

Gentiakochianin (Swertianine), an anthrone from Gentianaceae, has vasodilatory activity, induces glioma cell cycle arrest in the G(2)/M phase and inhibits proliferation, significantly reduces oxLDL-induced cell damage in EA.hy926 cells, inhibits ROS levels and up-regulated the activity of Akt/CREB/eNOS signaling pathway inhibited by oxLDL.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.