PI3K Activator

Doxycycline-d₃ hydrochloride is deuterium labeled Doxycycline hydrochloride (HY-N0565A). Doxycycline hydrochloride is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hydrochloride 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 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 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 has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.

Doxycycline-¹³C,d₃ is ¹³C and deuterium labeled Doxycycline (HY-N0565). Doxycycline is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline 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 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 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 has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.

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

PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (K_D: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC₅₀: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8⁺ T cells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cell proliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates T cell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1.

CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

MRS2768 is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

Hypoglycemic agent 3 (Compound H26), a derivative of corosolic acid, exhibits lipid-lowering and significant hypoglycemic effects and can be used as a hypoglycemic agent. Hypoglycemic agent 3 inhibits insulin resistance by targeting MCCC1 and can be used in the study of type 2 diabetes.

Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

(22S,23S)-Homobrassinolide (Standard) is the analytical standard of (22S,23S)-Homobrassinolide. This product is intended for research and analytical applications. (22S,23S)-Homobrassinolide is one of the most active brassinosteroids in inducing plant growth in various plant bioassay systems. (22S,23S)-Homobrassinolide shows Akt-dependent anabolic activity in rat skeletal muscle cells. Orally active[1].

20-5,14-HEDE-d₂ (WIT003-d₂) is the deuterated-labeled 20-5,14-HEDE (HY-160099). 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.

Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

SP6 exertes an antihypertensive effect through vascular NO regulation.

(+)-Licarin (Compound 7) is a compound derived from Ocotea macrophylla Kunth. leaves octanoid neolignans.

Hydroxyflutamide (Standard) (HFT (Standard)) is the analytical standard of Hydroxyflutamide (HY-W013272). This product is intended for research and analytical applications. Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC₅₀ of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.

Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.

Vasicine (hydrochloride) (Standard) is the analytical standard of Vasicine (hydrochloride). This product is intended for research and analytical applications. Vasicine hydrochloride (peganine hydrochloride) is a quinazoline alkaloid isolated from Justicia adhatoda. Vasicine hydrochloride activates PI3K/Akt signaling pathway, exhibits antioxidant, anti-inflammatory and antibacterial activities.

20-5,14-HEDE-d₂ (WIT003-d₂) is the deuterated-labeled 20-5,14-HEDE (HY-160099). 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.

1-Monopalmitin (Glyceryl palmitate) (Standard) is the analytical standard of 1-Monopalmitin (HY-W009141). This product is intended for research and analytical applications. 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells.

T3 Peptide is an active fragment of tumstatin. T3 Peptide binds integrin α_vβ₃/α_vβ₅, activates the PI3K/Akt/p70S6K signaling pathway, and thus stimulates the proliferation and migration of rat cardiac fibroblasts.

Umckalin is Coumarin (HY-N0709) derivative that exhibits anti-inflammatory properties. Umckalin reduces phosphorylation of p38 MAPK, JNK, and ERK, lowers TNF-α, IL-6, IL-1β, NO, and PGE₂ production. Umckalin can be used for the research of chronic inflammatory diseases.