PI3K Activator

Doxycycline is an orally active, broad-spectrum tetracycline antibiotic that also functions as an MMP inhibitor, exhibiting antibacterial, antiviral, antiparasitic, and antitumor activities. Doxycycline can bind to the classical binding site (CBS) within the mRNA decoding center of the bacterial 70S ribosome's 30S small subunit.Doxycycline blocks bacterial protein synthesis and inhibits the degradation of the extracellular matrix through its interaction with zinc and calcium ions. Doxycycline also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline 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 can disrupt transthyretin (TTR) amyloid fibrils. Doxycycline 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 can be used in research related to cancers—such as breast, prostate, and bladder cancer—as well as neurological disorders.

Doxycycline hyclate (Doxycycline (hydrochloride hemiethanolate hemihydrate); WC2031) is an orally active, broad-spectrum tetracycline antibiotic that also functions as an MMP inhibitor, exhibiting antibacterial, antiviral, antiparasitic, and antitumor activities. Doxycycline hyclate can bind to the classical binding site (CBS) within the mRNA decoding center of the 30S small subunit of the bacterial 70S ribosome.Doxycycline hyclate blocks bacterial protein synthesis and inhibits the degradation of the extracellular matrix through its interaction with zinc and calcium ions. 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 can disrupt transthyretin (TTR) amyloid fibrils. 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 can be used in research related to cancers—such as breast, prostate, and bladder cancer—as well as neurological disorders.

740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.

Doxycycline hydrochloride is an orally active, broad-spectrum tetracycline antibiotic that also functions as an MMP inhibitor, exhibiting antibacterial, antiviral, antiparasitic, and antitumor activities. Doxycycline hydrochloride can bind to the classical binding site (CBS) within the mRNA decoding center of the 30S small subunit of the bacterial 70S ribosome.Doxycycline hydrochloride blocks bacterial protein synthesis and inhibits the degradation of the extracellular matrix through its interaction with zinc and calcium ions. Doxycycline hydrochloride also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hydrochloride 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 hydrochloride can disrupt transthyretin (TTR) amyloid fibrils. Doxycycline hydrochloride 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 hydrochloride can be used in research related to cancers—such as breast, prostate, and bladder cancer—as well as neurological disorders.

Hyaluronic acid is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid is a major component of the extracellular matrix (ECM). Hyaluronic acid is synthesized at the plasma membrane. Increased hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid activates the PI3K-Akt signaling. Hyaluronic acid acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid can be studied in joint diseases, wound healing and cancer.

Hyaluronic acid sodium (Sodium hyaluronate) is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). Hyaluronic acid sodium is synthesized at the plasma membrane. Increased hyaluronic acid sodium levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid sodium participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid sodium activates the PI3K-Akt signaling. Hyaluronic acid sodium acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid sodium can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid sodium can be studied in joint diseases, wound healing and cancer.

Gamma-glutamylcysteine (γ-Glu-Cys) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.

UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC₅₀ value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush.

Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability.

Recilisib (ON 01210) is a radioprotectant, which can activate AKT, PI3K activities in cells.

Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia.

4-Vinylcyclohexene dioxide (4-Vinylcyclohexene diepoxide) is an orally active metabolite of 4-vinylcyclohexene. 4-Vinylcyclohexene dioxide induces Apoptosis, increases intracellular ROS, and activates the PI3K/Akt/mTOR pathway. 4-Vinylcyclohexene dioxide selectively damages small ovarian follicles, inhibits granulosa cell function, and disrupts the male reproductive system. 4-Vinylcyclohexene dioxide can be used in the study of premature ovarian insufficiency, reproductive toxicity, and related fertility disorders.

1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.

Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.

Heptadecanoic acid is an odd-chain saturated fatty acid (OCS-FA) with oral activity. Heptadecanoic acid can inhibit cell proliferation and induce Apoptosis. Heptadecanoic acid has antitumor activity. Heptadecanoic acid is associated with a number of diseases, including coronary heart disease, pre-diabetes and type 2 diabetes, and multiple sclerosis.

Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.

WS6 is an IkB kinase and EBP1 inhibitor, with IC₅₀ values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats^[1][2][4].

YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.

N6-Cyclohexyladenosine is a selective adenosine A1 receptor agonist (EC₅₀ = 8.2 nM). N6-Cyclohexyladenosine enhances the activation of the PI3K/Akt/CREB/BDNF axis. N6-Cyclohexyladenosine promotes remyelination, induces sleep, and improves 3-NP-induced Huntington's disease. N6-Cyclohexyladenosine can be used in liver cancer research.

SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways.