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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.
Tilorone is an orally active antiviral agent and interferon inducer that also has potential antineoplastic, immunomodulatory, and metabolic modulating effects. Tilorone induces an abnormally delayed interferon response and primarily stimulates interferon production in lymphoid tissue. Thus, Tilorone exerts antiviral effects and can be used as a chemotherapeutic agent. Tilorone has the potential to inhibit type 2 diabetes by increasing glucose uptake in vivo and in skeletal muscle cells by enhancing Akt2/AS160 signaling and glucose transporter levels.
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.
Tizanidine, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
KP372-1 is an Akt inhibitor that inhibits proliferation and induces apoptosis and anoikis. KP372-1 is also an NQO1 redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used in cancer research (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer).
Sophocarpine monohydrate is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine monohydrate upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine monohydrate inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine monohydrate can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine monohydrate has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
Gomisin D is an orally active lignan that binds to PDGFRβ with a Kd of 10 μM. By targeting PDGFRβ to regulate signaling pathways, Gomisin D inhibits the activation and proliferation of hepatic stellate cells and promotes their apoptosis, thereby ameliorating hepatic fibrosis. Gomisin D exhibits multiple activities such as photoprotection, antimelanogenesis, antioxidant effects, and hypoglycemic activity. Gomisin D can be used in studies related to diabetes, Alzheimer's disease, and hepatic fibrosis.
(-)-Syringaresinol is an orally active isomer of syringaresinol (HY-N8307) found in Annona Montana. (-)-Syringaresinol exhibits antioxidant, anti-inflammatory, and anticancer activities. (-)-Syringaresinol can alleviate ulcerative colitis via the PI3K-Akt/MAPK/Wnt signaling pathway. (-)-Syringaresinol inhibits HL-60 cell proliferation by arresting the G1 phase and inducing apoptosis. (-)-Syringaresinol inhibits LPS (HY-D1056)-induced microglial activation by downregulating the NF-κB p65 signaling pathway and its interaction with ERβ, exerting anti-neuroinflammatory effects.
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role.
Tenacissoside H (Tenacissimoside C) is a compound found in Caulis Marsdeniae Tenacissimae. Tenacissoside H shows anti-inflammation, anti-tumor and neuroprotective effects. Tenacissoside H inhibits PI3K/AktandNF-κB signaling pathway. Tenacissoside H inhibits cancer cells proliferation, S phase arrest, and inhibits tumor growyh in mice. Tenacissoside H promotes neurological recovery of ischemia-reperfusion injury in mice by inhibiting inflammation and apoptosis. Tenacissoside H can be used for the research of cancer, inflammation and neurological diseases, such as esophageal cancer and cerebral ischemia.
Tetrahydroalstonine ((-)-Tetrahydroalstonine) is an indole alkaloid and a selective α₂-adrenergic receptor antagonist. Tetrahydroalstonine exhibits certain neuroprotective effects. Tetrahydroalstonine can regulate autophagy-lysosomal function by activating the Akt/mTOR pathway, significantly reducing OGD/R-induced primary cortical neuronal injury.
CDPPB is a selective, orally active and brain-penetrant mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNFmRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease.
Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer.
Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate (HY-N0565B). This product is intended for research and analytical applications. Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.
DTPD-Q is an antioxidant and an oxidative derivative of methylbenzenesulfonyl-p-phenylenediamine DTPD. DTPD-Q is a molecule that binds to AKT1 and ESR1, with high binding affinity to core targets associated with male infertility and its subtypes. DTPD-Q can be used in studies related to male infertility.
Cyanidin 3,5-diglucoside chloride is an anthocyanin. Cyanidin 3,5-diglucoside chloride inhibits inflammatory cytokines (IL-1α, IL-1β, and IL-6) expression and NO production. Cyanidin 3,5-diglucoside chloride inhibits the phosphorylation of STAT3, IκB, ERK, p38, and AKT. Cyanidin 3,5-diglucoside chloride inhibits high pressure-induced decrease in GLAST. Cyanidin 3,5-diglucoside chloride exerts anti-inflammatory and skin barrier modulating effects. Cyanidin 3,5-diglucoside chloride can be used in retinal research.
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate 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.
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.
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