akt activity

(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) (20-Epiprotopanaxadiol), an apoptosis inducer, is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin.

AKT Kinase Inhibitor is an Akt inhibitor with antitumor activity that selectively inhibits cell proliferation in a dose-dependent manner.

Nimbolide suppresses CDK4/CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

SC79 is an AKT agonist with specificity and blood-brain barrier permeability. SC79 specifically binds to the PH domain of AKT, activates cytoplasmic AKT, and inhibits AKT membrane translocation. SC79 has neuroprotective activity.

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.

AKT Kinase Inhibitor HCl is an Akt inhibitor with antitumor activity.

RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. It exhibits anticancer activity and is a potential treatment for lung adenocarcinomas. RU-SKI 43 reduces Gli-1 activation through smoothening-independent non-canonical signaling and inhibits Akt and mTOR pathway activity.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

MMPP is a novel VEGFR2 inhibitor with anti-inflammatory and potential anticancer activity, inhibits STAT3, inhibits angiogenesis via VEGFR2/AKT/ERK/NF-kappaB pathway, and can be used to alleviate myocardial injury.

MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.This compound is unstable in powder form and other related salt forms are recommended.

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.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

BBO-10203 is an orally active small molecule, also designated as Compound 758, that functions as a selective PI3Kα-Ras interaction disruptor by binding to the Ras-binding domain of PI3Kα. BBO-10203 effectively prevents Ras-PI3Kα complex formation, inhibits downstream Akt activation without altering basal PI3Kα kinase activity, thereby minimizing risks of hyperglycemia and hyperinsulinemia, and displays selective antitumor activity against KRAS-mutant malignancies, making it an important investigational candidate for targeted cancer therapeutics.

RLX (PD 139530) is a PI3K/Akt/FoxO3a signal inhibitor with anticancer activity against tumour cell lines such as colon cancer, inducing sub-G1 arrest and mitochondrial potential loss, thereby inhibiting tumour growth. RLX also exhibits antitussive and anti-asthmatic activity, reducing eosinophils and total lymphocytes in bronchoalveolar lavage (BAL) fluid, and exhibits toxicity toward A549 cells.

RLX HCl is a narcissus ketone analogue with anticancer activity that inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a signalling pathway in experimental colon cancer, downregulating the p110α and p85 subunits of PI3K in HCT-116 cells, and exhibiting antiproliferative effects.

iHCK-37 (ASN05260065) is a selective Hck inhibitor with antitumor activity, blocking HIV-1 viral replication. iHCK-37 reduces PI3K/AKT and MAPK/ERK pathway activation after erythropoietin induction in high Hck-expressing cells, useful in chronic myelogenous leukemia (CML) research.

Imofinostat (MPT0E028) is a selective, orally available pan-HDAC inhibitor with IC₅₀ values of 53.0/106.2/29.5 nM against HDAC1/HDAC2/HDAC6 in HCT116 cells. In B-cell lymphoma, Imofinostat induces cell cycle arrest and apoptosis whilst inhibiting Akt phosphorylation, demonstrating anticancer activity across multiple tumour types.

AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1

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.

MSI-1701, an analogue of MSI-1436, enhances (MSI-1436) activity by increasing (pMEK) and (pERK) phosphorylation, thus promoting (PI3K/AKT) pathway signaling and inhibiting apoptosis in neuronal cells, which may contribute to its neuroprotective effects.

Coenzyme Q0 (CoQ0), a potent, orally active ubiquinone compound derived from Antrodia cinnamomea, induces apoptosis and autophagy. It suppresses HER-2/AKT/mTOR signaling, enhancing apoptosis and autophagy mechanisms. Additionally, Coenzyme Q0 regulates NFκB/AP-1 activation and promotes Nrf2 stabilization, contributing to the attenuation of inflammation and redox imbalance. It also exhibits anti-angiogenic activity by downregulating MMP-9/NF-κB and upregulating HO-1 signaling.