pakt

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

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

EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC₀ values of 0.16 μM for EGFRDel19, 21.73 μM for EGFR WT, and 41.56 μM for EGFRL858R. This compound exhibits anticancer activity across various cancer cell lines. EGFR-IN-154 induces mitochondrial apoptosis, reduces pERK1/2 and pAkt levels, and increases pJNK and pp38 levels.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

AM-0687 is a potent and selective PI3Kδ inhibitor. AM-0687 has Cellular potency: pAKT IC50 = 0.7 nM; HWB, u (pAKT) IC 50 = 4.6 nM. Rat KLH: IgG ED50 -= 0.026 mg/kg; IgM ED50 = 0.016 mg/kg. Rat PK Clu = 2.3 L/hr/kg.

AM-1430 is a potent and selective PI3Kδ inhibitor. AM-1430 has cellular potency: pAKT IC50 = 0.8 nM; HWB,u (pAKT) IC 50 = 7.7 nM. Rat KLH: IgG ED50 -= 0.016 mg/kg; IhM ED50 = 0.015 mg/kg. Rat PK Clu = 1.7 L/hr/kg.

RMC-5552 is a potent and selective inhibitor of mTORC1 that blocks phosphorylation of downstream signaling targets pS6K and p4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows markedly reduced inhibition of pAKT (IC50 19 nM), achieving approximately 40-fold selectivity for mTORC1 over mTORC2. RMC-5552 has demonstrated anticancer activity, supporting its potential use as a therapeutic agent in oncology and as a research tool for dissecting mTOR signaling pathways.

Dihydrocurcumin is the main metabolite of curcumin, which can reduce fat accumulation and oxidative stress response. Dihydrocurcumin can regulate the mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increase the protein expression levels of pAKT and PI3K, and reduce the intracellular NO and ROS contents through Nrf2 signaling pathway.

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