p-akt

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

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.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

1. Ilexsaponin A (Ilexsaponin A1) shows protective effects on ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway.

Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

Vevorisertib trihydrochloride (ARQ 751 trihydrochloride) is a selective and potent inhibitor of pan-AKT and AKT1-E17K mutations, inhibiting AKT1, AKT2 and AKT3. Vevorisertib trihydrochloride is used in the study of hepatocellular carcinoma and advanced solid tumours.

Saxagliptin (BMS-477118) is a selective, reversible DPP4 inhibitor with an IC50 of 26 nM.

Cichoric Acid (Dicaffeoyltartaric acid) is a potent inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase and the replication in tissues. It also a class of cannabinomimetics with CB2 receptor-dependent and independent.

Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase/AKT/mTOR pathway and delays sensitive cells in late mitosis.

Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.

NVP-BAG956 (BAG956) is a potent PI3K/PDK inhibitor that inhibits PI3Kδ, PI3Kα, PI3Kγ, and PI3Kβ, shows strong cytotoxicity against T-ALL cell lines, and can be used to study melanoma.

Triciribine phosphate (VD 002) is a highly selective AKT inhibitor that induces cell cycle arrest and cysteinyl asparagin-dependent apoptosis, inhibits neovascularization, and can be used in the study of leukemia.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

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.

4-Hydroxybenzyl alcohol (P-Methylolphenol) exhibits beneficial effects in cerebral ischemic injury, has neuroprotective effect through upregulation of Nrf2, Prdx6, and PDI expression via the PI3K/Akt pathway. 4-Hydroxybenzyl alcohol inhibit the development of new blood vessels by targeting multiple mechanisms of the angiogenic process, may as a promising candidate for the establishment of anti-angiogenic treatment strategies in cancer therapy.