Akt Inhibitor

Leupeptin hydrochloride is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis.

Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

BMS-554417 is an orally active inhibitor of insulin receptor and insulin-like growth factor-I receptor (IGF-1R) kinases, with IC₅₀ values of 50.6 nM and 67.9 nM, respectively. BMS-554417 blocks downstream signal transduction via the ERK and PI3K/Akt pathways. BMS-554417 induces G0-G1 cell cycle arrest, prevents cyclin D1 accumulation in the nucleus, triggers mitochondrial pathway-mediated apoptosis, promotes HER2 phosphorylation, and inhibits the proliferation and growth of cancer cells. BMS-554417 can be used in research related to colon cancer, ovarian cancer, and breast cancer.

Liriodendrin is an orally effective lignan compound with anti-inflammatory, antioxidant, and anti-platelet aggregation activities. Liriodendrin is isolated and extracted from Sargentodoxae caulis and Linaria vulgaris. Liriodendrin regulates the expression of genes related to inflammation and cellular metabolism by inhibiting the NF-κB, PI3K/Akt, and TLR4 signaling pathways, or by activating the PI3K-DDX18 pathway. Liriodendrin increases the expression of HSF1 and HSP27 without cytotoxicity. Liriodendrin is used in studies on ulcerative colitis, myocardial ischemia-reperfusion injury, sepsis-induced acute lung injury, and chronic endometritis.

Pancracine is an alkaloid. Pancracine upregulates p27, phosphorylated p38 MAPK and phosphorylated p53, while downregulating phosphorylated Akt and phosphorylated Rb. Pancracine induces G₁ cell cycle arrest and Apoptosis in cells. Pancracine inhibits the replication of pseudotyped HIV-1 and Dengue virus. Pancracine can be used in research related to lung adenocarcinoma, acute lymphoblastic leukemia, cutaneous epidermoid carcinoma, human immunodeficiency virus infection and dengue virus infection.

Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42).

Sapanisertib (INK-128; MLN0128; TAK-228) Standard is the analytical standard of Sapanisertib (HY-13328). This product is intended for research and analytical applications. Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

Bruceoside B is a PI3K/Akt/NF-κB inhibitor. Bruceoside B reduces LPS (HY-D1056)-induced nitric oxide release and the secretion of TNF-α, IL-6 and IL-1β, and decreases the activation level of apoptosis. Bruceoside B inhibits the replication, coat protein accumulation and local lesion formation of tobacco mosaic virus (TMV), and enhances the anti-infection ability of plants. Bruceoside B can be used in studies related to acute lung injury and tobacco mosaic virus infection.

Honokiol (Standard) is the analytical standard of Honokiol. This product is intended for research and analytical applications. Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.

Guaiazulene (Standard) is the analytical standard of Guaiazulene (HY-N6951). This product is intended for research and analytical applications. Guaiazulene is a bicyclic sesquiterpene that can cross the blood-brain barrier. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.

ML-7 is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition. As a non-antibiotic adjuvant, ML-7 restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117). ML-7 can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection.

Etilefrine (Standard) is the analytical standard of Etilefrine. This product is intended for research and analytical applications. Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.

4-Hydroxychalcone (Standard) is the analytical standard of 4-Hydroxychalcone (HY-107818). This product is intended for research and analytical applications. 4-Hydroxychalcone is an orally active flavonoid precursor. 4-Hydroxychalcone inhibits VEGF- and bFGF-induced phosphorylation of ERK1/2 and Akt. 4-Hydroxychalcone suppresses resistant hypertension by alleviating hyperaldosteronism, inflammation and renal injury in cryptochrome gene knockout mice. 4-Hydroxychalcone possesses anti-angiogenic activity.

Jervine hydriodide (11-Ketocyclopamine hydriodide) is an orally active steroidal alkaloid and Hedgehog signaling pathway inhibitor. Jervine hydriodide can be isolated from Veratrum californicum. Jervine hydriodide regulates Wnt, inhibits the AKT/mTOR signaling pathway, and activates the AMPK signaling pathway. Jervine hydriodide induces DNA damage, Apoptosis, Autophagy, ROS production and Mitochondrial damage. Jervine hydriodide exhibits anti-cancer and anti-inflammatory activities. Jervine hydriodide reduces tumor growth rate and weight in xenograft models. Jervine hydriodide can be used in studies related to triple-negative breast cancer, nasopharyngeal carcinoma and non-small cell lung cancer.

Molephantin is a blood-brain barrier permeable anti-glioblastoma compound. Molephantin induces ROS generation, leading to mitochondrial damage, Mitophagy flux blockage and Apoptosis induction. Molephantin can suppress the PI3K/Akt/mTOR signaling pathway. Molephantin demonstrates antitumor effects against glioblastoma.

M2698 (Standard) is the analytical standard of M2698 (HY-100501). This product is intended for research and analytical applications. M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

Lixisenatide (Leu-¹³C₆,¹⁵N) TFA is the ¹³C- and ¹⁵N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.

MK-2206 dihydrochloride (MK-2206 2HCl) (Standard) is the analytical standard of MK-2206 dihydrochloride (HY-10358). This product is intended for research and analytical applications. MK-2206 dihydrochloride is an orally active pan-AKT inhibitor, with IC₅₀ values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia.

BAY1125976 (Standard) is the analytical standard of BAY1125976 (HY-100018). This product is intended for research and analytical applications. BAY1125976, a chemical probe, is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.