Akt

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.

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

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44 42 MAPK.

Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3 Girdin Akt signaling in HCC cells.

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.

1. Herbacetin induces apoptosis in HepG2 cells, by ROS and PI3K Akt pathway. 2. Herbacetin suppresses the HGF-induced motility of human breast cancer MDA-MB-231 cells by inhibiting c-Met and Akt phosphorylation.

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.

α-Linolenic Acid (ALA) is an essential fatty acid that cannot be synthesized by the human body and is obtained by isolating it from seed oils. α-Linolenic acid has been shown to improve memory, inhibit thrombosis, and lower blood lipids.

Akt3 degrader 1 is a specific Akt3 degrader with anticancer and antiproliferative activity that inhibits tumor growth in mice.Akt3 degrader 1 is used in the study of non-small cell lung cancer and pancreatic cancer.

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.

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).

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.

TIC10 (ONC-201) inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1 2.

(Z)-Guggulsterone inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.

Isobavachalcone (Corylifolinin) is a chalcone constituent of Angelica keiskei, has potent anti-inflammatory activity, possible can ameliorate neuronal injury in brain diseases associated with inflammation.

Ipatasertib (GDC-0068) is a selective, ATP-competitive pan-Akt inhibitor that inhibits Akt1 (IC50:5 nM), Akt2 (IC50:18 nM), and Akt3 (IC50:8 nM). Ipatasertib (GDC-0068) can lead to p53-independent PUMA activation by inhibiting Akt, thereby activating FoxO3a and NF-κB simultaneously, directly binding to the PUMA promoter, upregulating PUMA transcription and Bax-mediated intrinsic mitochondrial apoptosis.

Oridonin (NSC-250682) is a diterpenoid isolated from Rabdosia rubescens with anti-tumor, anti-bacterial and anti-inflammatory effects. It acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

BAY1125976 is an allosteric inhibitor of Akt1 and Akt2 (IC50s of 5.2 and 18 nM, respectively, in a time-resolved FRET assay)

Chrysoeriol has antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities, it also shows selective bronchodilator effect.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1 2 3, p70S6K, PKA, and ROCKI II.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

YS-49 is an activator of PI3K Akt (a downstream target of RhoA).

Recilisib (ON 01210) is a radioprotectant that activates AKT and PI3K activities in cells.

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

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

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

N-Feruloyloctopamine is a natural product.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

1,3-Dicaffeoylquinic acid (CYNARIN) is a natural product. It shows antioxidant and choleretic properties and is a potential immunosuppressive agent.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu

BX517 (PDK1 inhibitor 2) is a potent and selective inhibitor of PDK1.

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.

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective, ATP-competitive inhibitor of pan-Akt, with IC50 values of 5 nM, 18 nM, and 8 nM for Akt1, Akt2, and Akt3, respectively.

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

1. Phellodendrine (Phallodendrin) has anti-nephritic activity, may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.

Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.

Pachymic acid (3-O-Acetyltumulosic acid) is a natural product, and inhibits Akt and ERK signaling pathways.

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

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.

N-Oleoyl Glycine, a Lipoamino Acid, Stimulates Adipogenesis Associated With Activation of CB1 Receptor and Akt Signaling Pathway in 3T3-L1 Adipocyte

Artemisinin (Qinghaosu) is a natural product, a sesquiterpene lactone, derived from Artemisia annua. Artemisinin has anti-malarial activity, as well as neuroprotective and anti-tumor activity.

Arnicolide D is a sesquiterpene lactone. Arnicolide D isolates from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K AKT mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner. Arnicolide D exerts strong cytotoxic activity on the human colon carcinoma HT-29 cell line.

Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

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.