Src Activator

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC₅₀ of 63 nM.

EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.

Propionyl-L-carnitine is an orally active L-carnitine derivative. Propionyl-L-carnitine has a high affinity for muscle L-carnitine transferase. Propionyl-L-carnitine increases Apoptosis, Bax, and reduces NF-κB, VCAM-1, MCP-1, and survivin. Propionyl-L-carnitine activates Src kinase, Akt, induces p-AMPK and nitric oxide synthesis. Propionyl-L-carnitine alleviates cardiovascular disease, obesity, and colitis.

Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling.

15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC₅₀=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC₅₀=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC₅₀=320 ng/mL).

MRS2768 tetrasodium salt is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 tetrasodium salt activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 tetrasodium salt inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 tetrasodium salt activates eNOS to increase NO secretion in endothelial cells. MRS2768 tetrasodium salt drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 tetrasodium salt exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 tetrasodium salt 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.

Convulxin is a toxin found in a tropical rattlesnake. Convulxin stimulates platelet aggregation, and clusters GPVI to trigger Src family kinase activation, Fc receptor γ chain phosphorylation, and p72SYK signaling. Convulxin interacts with Dectin-2 to induce IL-10 production, activates monocytes to generate ROS and NLRP3 inflammasome-mediated IL-1β secretion, and induces mitochondrial ROS. Convulxin causes transient arterial blood pressure changes in dogs. Convulxin can be used for research related to coagulation.

15-Deoxy-Δ12,14-Prostaglandin D2-d₄ (15-Deoxy-Δ12,14-PGD2-d₄) is the deuterium labeled 15-deoxy-Δ12,14-Prostaglandin D2. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is a metabolite of prostaglandin D₂ (PGD₂) (HY-101988), which can undergo further dehydration metabolism to 15-deoxy-Δ12,14-PGJ₂. 15-deoxy-Δ12,14-Prostaglandin D2 is a highly selective agonist for DP2 receptor and PPARγ. 15-deoxy-Δ12,14-Prostaglandin D2 causes morphological changes in eosinophils and migration of type II innate lymphoid cells (ILC2). 15-deoxy-Δ12,14-Prostaglandin D2 has a growth inhibitory effect on prostate cancer cells expressing PPARγ, induces cell cycle arrest and promotes apoptosis. 15-deoxy-Δ12,14-Prostaglandin D2 can be used in related research on asthma and prostate 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.