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Akt/PKB (Protein kinase B), a serine/threonine protein kinase with antiapoptotic activity, is one of the major downstream targets of PtdIns(3,4,5)P3 signaling pathway. It contains a pleckstrin homology domain (PH domain) that specifically binds PtdIns(3,4,5)P3 on the plasma membrane. Akt phosphorylation and activation are directly determined by the level of PtdIns(3,4,5)P3 on the plasma membrane, which is regulated by PI3K.
Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Akt isoforms have an N-terminal PH (pleckstrin homology) domain and a kinase domain, which are separated by a 39-amino-acid hinge region. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis.
Akt is a crucial mediator of cell survival and its deactivation is implicated in various stress-induced pathological cell death and degenerative diseases.
Etaracizumab (LM 609) is an αvβ3integrinIgG mAb. Etaracizumab is developed to target αvβ3+cancer cells via NK cell-mediated cytotoxicity. Etaracizumab sterically hinders access of large ligands to the RGD-binding pocket, without obstructing it. Etaracizumab decreases p-Akt in vitro. Etaracizumab can decrease cancer proliferation and invasion. Etaracizumab induces tumor cell apoptosis, and inhibition ofαvβ3-mediated cell adhesion, endothelial cell migration and osteoclast-mediated bone resorption. Etaracizumab can be studied in anti-tumor research against cancers such as ovarian cancer, metastatic melanoma as well as advanced solid tumors. Recommend Isotype Control: Human IgG1 kappa, Isotype Control (HY-P99001).
Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.
Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases.
UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3IC50 = 60 nM, AXLIC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.
Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders.
Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.
Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
Deferoxamine (mesylate) (Standard) is the analytical standard of Deferoxamine (mesylate). This product is intended for research and analytical applications. Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.
Atranorin is a secondary metabolite of lichens and AKT inhibitor. Atranorin possesses multiple activities such as antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Atranorin has IC50 values for scavenging DPPH and ABTS free radicals of 117 μM and less than 10 μM, respectively. Additionally, Atranorin also exhibits effects in promoting wound healing. Atranorin can be used in the research of various diseases, including myelodysplastic syndromes, tumors, and inflammatory conditions.
Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
Naphthazarin (DHNQ) is a microtubule depolymerizing agent. Naphthazarin can improve motor function and reduce neuroinflammation in mouse models of Parkinson's disease. Naphthazarin can induce tumor cell apoptosis, autophagy, and cell cycle arrest. Naphthazarin can also induce erythrocyte apoptosis. Naphthazarin can be used in the research of tumors and neurodegenerative diseases.
Revaprazan hydrochloride is reversible proton pump inhibitor. Revaprazan hydrochloride can inhibit gastric acid secretion and protect gastric mucosa. Revaprazan hydrochloride can inhibit IkappaB-alpha degradation as well as Akt inactivation, resulting in attenuation of H. pylori-induced COX-2 expression. Revaprazan hydrochloride can be used for the researches of infection and inflammmation, such as H. pylori-infected gastric inflammation and gastric ulcer.
6'-Sialyllactose promotes the growth of beneficial bacteria (such as Bifidobacterium and lactobacillus) and inhibits the proliferation of harmful bacteria. 6'-Sialyllactose exhibits anti-inflammatory and anti-angiogenic activities. 6'-Sialyllactose promotes the muscle health.
20-5,14-HEDE (WIT003) is an analog of 20-HETE. 20-5,14-HEDE activates PI3K/Akt signaling pathway, thereby exhibiting anti-apoptotic and cell survival promoting effects. 20-5,14-HEDE is the agonist for 20-HETE that increases intracellular Ca2+ concentrations, thereby enhancing vasoconstriction.
Benazepril (CGS14824A) hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy.
