pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan- HER inhibitor. pan-HER-IN-1 exhibits IC 50s of 0.38, 1.6, 2.2 and 3.5 nM for EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and exhibits antitumor activities.

Pembrolizumab is a humanized monoclonal antibody inhibiting the PD-1 receptor and the first in the class of agents called the HER2 dimerization inhibitors that impairs the ability of HER2 to bind to other members of the HER family.

PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.

Coenzyme Q0 (CoQ0), a potent, orally active ubiquinone compound derived from Antrodia cinnamomea, induces apoptosis and autophagy. It suppresses HER-2/AKT/mTOR signaling, enhancing apoptosis and autophagy mechanisms. Additionally, Coenzyme Q0 regulates NFκB/AP-1 activation and promotes Nrf2 stabilization, contributing to the attenuation of inflammation and redox imbalance. It also exhibits anti-angiogenic activity by downregulating MMP-9/NF-κB and upregulating HO-1 signaling.

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

SU-4312, also known as DMBI, is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 values are 0.8 and 19.4 μM respectively). SU4312 (SU 4312) unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS.

(-)-Epigallocatechin Gallate (EGCG) is an antioxidant polyphenol flavonoid that inhibits telomerase and DNA methyltransferase. (-)-Epigallocatechin Gallate (EGCG) blocks the activation of EGF receptors and HER-2 receptors. (-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant found in a number of plants such as green and black tea. It inhibits cellular oxidation and prevents free radical damage to cells.

PROTAC Her3 Degrader-8 (Compound PP2) is a proteolysis targeting chimera (PROTAC) capable of degrading the Her3 protein in vitro and within cellular assays, with potential to investigate diseases modulated by HER family proteins [1].

XMT-1519 conjugate-1 (compound 31) serves as a linker for the HER-2 monoclonal antibody XMT-1519, facilitating the synthesis of antibody-drug conjugates (ADCs) to enhance antitumor activity [1].

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.