EGFR Modulator

EGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR.

Neoschaftoside is a C-glycosyl flavonoid EGFR modulator, antifungal agent, and piercing-sucking stimulant for planthoppers. Neoschaftoside forms stable EGFR complexes, restricts global protein movement, enhances related dynamic processes, and inhibits tumor progression. Neoschaftoside interacts with EGFR core regulatory genes associated with lung cancer. Neoschaftoside inhibits Botrytis cinerea. Neoschaftoside can be used in research related to lung cancer and Botrytis cinerea infections.

SU-4313 is a potent protein tyrosine kinases (PTKs) modulator with IC₅₀s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation.

CHNQD-01281, a derivative of Brefeldin A (HY-16592), is a EGFR modulator. CHNQD-01281 has strong antiproliferative activities against cancer cells (IC₅₀: 0.079 and 0.081 μM for T24 and J82 cells, respectively). CHNQD-01281 regulates both EGFR/PI3K/AKT and EGFR/ERK pathways and mediates the chemotactic effect of chemokines on immune effector cells. CHNQD-01281 remarkably inhibits tumor growth in T24 xenograft mice model and prolongs the survival time in MB49 allogeneic mice model via inducing infiltration of cytotoxic T cells.

IGF-1R modulator 1 (Example 5) is an IGF-1R modulator, with EC₅₀s of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), 0.39 μM (TrkB). IGF-1R modulator 1 can be used for research of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease.

Eucommin A is a natural polyphenolic antioxidant. Eucommin A forms stable complexes with EGFR and MAPK8 via hydrogen bonding and hydrophobic interactions, and regulates osteoarthritis-related Autophagy. Eucommin A is applicable to research related to oxidative stress, such as osteoarthritis.