Src

Chrysotoxine is a dual inhibitor of the Src and Akt signaling pathways. It effectively suppresses cancer stem cell phenotypes by down-regulating the Src/Akt pathway, leading to reduced cell viability and increased apoptosis in H460 and H23 cancer cell lines, while sparing non-tumor cell lines. Due to its rapid excretion and low bioavailability in animal studies, Chrysotoxine serves as a valuable tool in cancer research, particularly for investigating therapies targeting cancer stem cells.

Si306 is a selective Src inhibitor known for its antitumor properties. It effectively reduces the phosphorylation of focal adhesion kinase (FAK) and downregulates the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM) cells. This compound is valuable for research focused on understanding Src-related signaling pathways and developing targeted cancer therapies.

SKS-927 is a potent Src kinase inhibitor with an IC50 value of 3.9 nM, demonstrating significant inhibition of Src-transformed cell proliferation in rat fibroblasts, with an IC50 of 73 nM. Additionally, SKS-927 shows activity against EGFR at an IC50 of 720 nM. This compound is applicable in research focused on cancer and osteoporosis, making it a valuable tool for investigating therapeutic pathways in these conditions.

β-Hydroxyisovalerylshikonin is a natural product derived from Lithospermum erythrorhizon, functioning as a potent Src inhibitor. It exhibits significant inhibitory activity against protein tyrosine kinases, with IC50 values of 0.7 μM for EGFR and 1 μM for the v-Src receptor. This compound demonstrates broad anticancer activity, particularly inducing cell death in various tumor cell lines, most notably in NCI-H522 and DMS114 cells, making it a valuable tool for cancer research applications.

(E/Z)-MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator that enhances SRC activity in cancer cells. This leads to the overstimulation of reactive oxygen species (ROS) production, resulting in cell stress and apoptosis through a mechanism known as paraptosis. (E/Z)-MCB-613 serves as a cytotoxic agent with significant implications for cancer research, particularly in studies focusing on targeted cancer therapies and mechanisms of cell death.

AZ12672857 is a potent inhibitor of EphB4 and Src kinases, demonstrating an IC50 of 1.3 nM for EphB4. This compound significantly inhibits the proliferation of c-Src transfected 3T3 cells with an IC50 of 2 nM and autophosphorylation of EphB4 in CHO-K1 cells with an IC50 of 9 nM. AZ12672857 can be utilized in studies investigating signaling pathways related to cancer and cell growth regulation.

Canine Secretin is an endocrine hormone that primarily targets the Src kinase pathway. It stimulates the secretion of bicarbonate-rich pancreatic fluids and regulates gastric chief cell function, as well as paracellular permeability in canine gastric monolayers. This reagent is valuable for research applications involving gastrointestinal physiology and pancreatic function in canines.

ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis.

SI-2 hydrochloride is a potent inhibitor of SRC-3, a transcription co-regulator involved in various signaling pathways. This compound displays favorable pharmacokinetic properties and reduced toxicity, making it suitable for in vivo studies. SI-2 hydrochloride is valuable for research related to cancer biology, endocrine signaling, and other conditions where SRC-3 plays a critical role.

(+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology.

TG 100948 is a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and tyrosine kinase Src. This compound demonstrates significant biological activity by reducing retinal edema and retinal thickening, as well as eliminating bullous edema cysts in rat models of ischemic retinal vein occlusion. TG 100948 is valuable for research into the pathophysiology and potential treatments of ischemic retinal vein occlusion.