homodimers

SR11237 is a Pan retinoid X receptor (RXR) agonist. SR11237 causes RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.

TWIK-1/TREK-1-IN-3 is a selective and potent inhibitor of the potassium channel TREK-1, effectively inhibiting TREK-1 homodimers and TWIK-1/TREK-1 heterodimers containing two-pore-domain potassium (K2p) channels. TWIK-1/TREK-1-IN-3 exhibits antidepressant activity and can be utilized in the study of depression.

TH023 is an inhibitor of the TLR4 signaling pathway, specifically targeting the formation of TLR4 homodimers. In HEK-Blue hTLR4 cells, TH023 suppresses the secretion of embryonic alkaline phosphatase with an IC50 of 0.354 μM and inhibits NO expression in RAW264.7 cells, with an IC50 of 1.61 μM. Additionally, TH023 inhibits the activation of NF-κB and reduces the nuclear translocation of NF-κB p65. The compound demonstrates anti-inflammatory effects in a mouse model of LPS-induced acute sepsis and improves lung injury in mice.

Nurr1 agonist 9 (Compound 36) acts as an agonist for Nurr1, with an EC50 of 0.090 µM and a Kd of 0.17 µM. It activates Nurr1 homodimers (NurRE, EC50 = 0.094 µM) and Nurr1-RXR heterodimers (DR5, EC50 = 0.165 µM). This compound induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in Parkinson's disease organoid models and can penetrate the human brain endothelial cell barrier.

MyD88-IN-4 is a MyD88 inhibitor. It exerts antiviral effects by upregulating IFN-β and demonstrates anti-inflammatory properties by inhibiting the production of pro-inflammatory cytokines. MyD88-IN-4 prevents the formation of MyD88 homodimers and interferes with its interaction with IRF3/IRF7. In a mouse model infected with VEEV TC-83, MyD88-IN-4 shows efficacy against encephalitic alphavirus infections by reducing viral replication and increasing survival rates. This compound is applicable for research on alphavirus infections, bacterial toxin-related diseases, and sepsis.

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR, with Ks values of 0.6 and 1.1 µM, respectively. It disrupts the stability of Nurr1 homodimers selectively while stabilizing Nurr1:RXR heterodimers, specifically activating the heterodimer response element DR5. In neuronal cells, Nurr1/RXR dual agonist 1 enhances the expression of neuroprotective Nurr1 target genes without inducing genes associated with off-target effects. This compound is applicable in studies related to neurodegenerative diseases.

Pegpleranib sodium is a polyethylene glycol-modified nucleic acid aptamer that specifically binds to the homodimers and heterodimers of PDGF-BB and PDGF-AB, thereby inhibiting their interaction with associated tyrosine kinase receptors.

Pegpleranib is a polyethylene glycol-modified nucleic acid aptamer that specifically binds to both homodimers and heterodimers of PDGF-BB and PDGF-AB, thereby inhibiting their interaction with associated tyrosine kinase receptors.

BMS-8 is a novel inhibitor of the PD-1/PD-L1 interaction (IC50: 7.2 μM) by binding directly to PD-L1 and inducing the formation of PD-L1 homodimers.

HX-603 is a selectivity agonist of RXR that inhibits the activation of RAR-RXR heterodimers as well as RXR homodimers.

Izalontamab (SI-B001) is a bispecific EGFR/HER3 monoclonal antibody that binds to both EGFR×EGFR homodimers and EGFR×HER3 heterodimers, thereby blocking downstream pathways. It is applicable for locally advanced or metastatic epithelial tumours, such as non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC).

Compound 2a, identified as TWIK-1/TREK-1-IN-1, acts as an inhibitor of the TREK-1, a two-pore domain potassium channel (K2p) that forms TREK-1 homodimers and TWIK-1/TREK-1 heterodimers, both significant for its role as an antidepressant target. Furthermore, TWIK-1/TREK-1-IN-3, a related compound, selectively inhibits these channels with IC50 values of 9.36 μM for TREK-1 homodimers and 14.6 μM for TWIK-1/TREK-1 heterodimers, demonstrating antidepressant-like effects [1].

COVA322 is a bispecific antibody targeting both TNF and IL-17A. It simultaneously inhibits TNF and IL-17A homodimers, making it useful for researching inflammatory diseases.

L2P4 TFA is a peptide-based fluorescent probe targeting EBNA1, capable of hindering the formation of EBNA1 homodimers and selectively suppressing the growth of EBV+ tumors. It demonstrates cytotoxicity in EBV-positive C666-1 cells, with an LC50 of 46.4 μM.