Akt Inhibitor

AKT inhibitor VIII (Standard) is the analytical standard of AKT inhibitor VIII (HY-10355). This product is intended for research and analytical applications. AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.

DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC₅₀ of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca²⁺/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.

Y-27632 (Standard) is the analytical standard of Y-27632 (HY-10071). This product is intended for research and analytical applications. Y-27632 is a ROCK inhibitor with K_i values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.

Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

Daphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.

Perillyl alcohol (Standard) is the analytical standard of Perillyl alcohol (HY-N7000). Perillyl alcohol is an orally active monoterpene. Perillyl alcohol exhibits multiple activities such as analgesic, anti-inflammatory, anti-tumor, anti-angiogenic, and anti-nociceptive effects. Perillyl alcohol can induce apoptosis and cell cycle arrest in tumor cells.

Monosialoganglioside GM3 (bovine) is a monosialoganglioside and an inhibitor of VEGFR2 and Akt. At a concentration of 20 μM, Monosialoganglioside GM3 inhibits angiogenesis and reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by inhibiting VEGFR2 and Akt phosphorylation. Ganglioside GM3 also inhibits ferroptosis, providing protective effects during the formation of abdominal aortic aneurysms. Additionally, Monosialoganglioside GM3 (bovine) acts as an inhibitor of insulin signaling, inducing the dissociation of the insulin receptor (IR)-Caveolin-1 complex from lipid microdomains and causing insulin resistance in adipocytes. Monosialoganglioside GM3 (bovine) can be used in cancer and metabolic disease research.

Urolithin B (Standard) is the analytical standard of Urolithin B. This product is intended for research and analytical applications. Urolithin B is one of Ellagitannins' slow microbial products, and has anti-inflammatory and anti-inflammatory effects. Urolithin B suppresses NF-κB activity. Urolithin B suppresses JNK, ERK and Akt's oxidation, and increases AMPK's oxidation. Urolithin B is also a quantitative change factor for bone and skin quality.

F16 (Standard) is the analytical standard of F16 (HY-100395). This product is intended for research and analytical applications. F16 is a mitochondrial permeability transition pore (PTP) modulator with an EC₅₀ of 30 μM in mice. F16 promotes PTP opening, accumulates in cancer cell mitochondria, and induces mitochondrial depolarization, swelling, cristae disruption, outer membrane rupture, ATP depletion, reactive oxygen species (ROS) production, cytochrome c release and mitochondrial uncoupling. F16 induces cell cycle arrest at the G1 (occasionally G2) phase, reduces the phosphotyrosine content of Neu, as well as the levels of phosphorylated PKB/Akt and phosphorylated MAP kinase, downregulates the protein expression levels of Neu and PKB, triggers apoptosis in cells with moderate Bcl-2 expression, and induces necrosis in cells with overexpressed Bcl-2. F16 can be used in research related to breast cancer and gastric cancer.

Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.

Schisantherin B (Gomisin-B) (Standard) is the analytical standard of Schisantherin B. This product is intended for research and analytical applications. Schisantherin B is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tau protein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression.

Cinnamyl Alcohol-d₉ is deuterated labeled Cinnamyl Alcohole (HY-Y0045). Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.

Petunidin-3-O-glucoside chloride (Standard) is the analytical standard of Petunidin-3-O-glucoside chloride (HY-N7832). This product is intended for research and analytical applications. Petunidin-3-O-glucoside chloride is a blood-brain barrier-penetrating tyrosinase inhibitor with an IC₅₀ of 10.3 μM and a K_i of 9.0 μM. Petunidin-3-O-glucoside also acts as an α-glucosidase inhibitor with an IC₅₀ of 218.2 µM. Petunidin-3-O-glucoside chloride inhibits the SIRT3/p53-mediated mitochondrial pathway and the PI3K/Akt-ERK pathway, suppresses glycolysis, and induces cell apoptosis. Petunidin-3-O-glucoside chloride scavenges ROS to exert antioxidant activity. It can be used in research related to glioblastoma multiforme, skin anti-aging and whitening, as well as obesity.

DZ2002 (Standard) is the analytical standard of DZ2002. This product is intended for research and analytical applications. DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

GSK-690693 (Standard) is the analytical standard of GSK-690693 (HY-10249). This product is intended for research and analytical applications. GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC₅₀s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.

Fenitrothion (Standard) is the analytical standard of Fenitrothion (HY-B1885). This product is intended for research and analytical applications. Fenitrothion is a broad-spectrum and orally active insecticide/acaricide. Fenitrothion inhibits cholinesterase, AMPKα and IRS1/PI3K/AKT. Fenitrothion causes Apoptosis, reduces SOD activity. Fenitrothion shows insecticidal effect against Rhyzopertha dominica and Tribolium castaneum adults. Fenitrothion is widely used in cotton crops, vegetable crops, fruit crops and field crops, especially rice. Fenitrothion can be used for brain and spleen toxicology studies.

Ethalfluralin is a dinitroaniline herbicide and microtubule inhibitor. Ethalfluralin blocks nuclear division and cytokinesis of parasites by inhibiting intranuclear spindle formation. Ethalfluralin activates the phosphorylation levels of NF-κB and P38 MAPK, inhibits the PI3K/AKT signaling pathway, impairs mitochondrial function, and induces apoptosis, endoplasmic reticulum stress, autophagy, and ROS production. Ethalfluralin is applicable to research related to toxoplasmosis.

DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC₅₀s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice.

Cilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

CNBDA is a selective SHP2 inhibitor with an IC₅₀ of 5 μM. CNBDA binds to the active site of SHP2 through interactions with surrounding positively charged and polar amino acids, inhibits the PTPase activity of SHP2, and blocks the autodephosphorylation of SHP2. CNBDA inhibits the transformed phenotype, proliferation, anchorage-independent growth, and mammosphere formation of breast cancer cells, as well as EGF-induced Ras-ERK and PI3K-Akt signaling pathways, downregulates HER2 expression, and induces cell death. CNBDA can be used in breast cancer-related research.