dimerization

Mycro 3 is potent and selective for c-Myc in whole cell assays.

BMS-1166 is a potent inhibitor of the PD-1/PD-L1 interaction.

Ochromycinone (STA 21) is a selective STAT3 inhibitor.

LQZ-7I is an inhibitor of surviving-targeting. It orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Pembrolizumab (MK-3475) is a highly selective humanized monoclonal antibody that antagonizes PD-1. It can block the PD-1 protein on T cells and prevent their interaction with PD-L1 on cancer cells.

Pertuzumab (anti-HER2) a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors impairs the ability of HER2 to bind to other members of the HER family.

GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.

Cucurbit[8]uril is a highly effective and safe supramolecular compound that promotes protein heterodimerization. It selectively induces the heterodimerization of methylviologen and naphthalene functionalized proteins, demonstrating its specificity and versatility. Additionally, Cucurbit[8]uril shows exceptional oral activity and low toxicity, making it a promising candidate for various pharmaceutical and biotechnological applications.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

VRT-325 is a CFTR modulator with the ability to promote ΔF508-CFTR folding and endoplasmic reticulum trafficking. VRT-325 restores chloride transport in bronchial epithelial cells from cystic fibrosis patients and accelerates healing of CF cell monolayers, used for experimental research in cystic fibrosis.

STX-0119 is a selective, orally active STAT3 dimerization inhibitor that suppresses STAT3 transcription with an IC50 of 74 μM.

2,5-Dihydroxybiphenyl (TFIIH Modulator12), a small molecule destabilization inducer, induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.

TFIIH Modulator-19 induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.

Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase at the endoplasmic reticulum (ER) and lysosomal pHs, increases lysosomal substrate metabolism, and has therapeutic potential for the treatment of Parkinson's and Gosheimer's diseases.

α-Truxillic acid, a dimer of α-trans-cinnamic acid, inhibits inflammatory pain responses.

(Rac)-IBT6A is a racemate of IBT6A, an impurity of Ibrutinib that can be utilized in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct.

AC-73 is an orally available Cluster of Differentiation 147 (CD147) inhibitor with high bioavailability that selectively disrupts the dimerization of CD147 (the binding site is in the N-terminal IgC2 domain of CD147 including Glu64 and Glu73), resulting in inhibition of the CD147/ERK1/2/STAT3/MMP-2 pathway and inhibition of liver cancer cell motility and invasion. AC-73 has antiproliferative activity and induces autophagy in leukemia cells.

ST 2825 is a specific MyD88 dimerization inhibitor that blocks IL-1β-mediated activation of NF-κB transcriptional activity.

ERBB agonist-1 (Compound EF-1) is an ERBB4 agonist (EC50=10.5 μM) that induces ERBB4 receptor dimerization and phosphorylation of Akt and ERK1/2. It exhibits cardioprotective effects in mouse models and prevents myocardial fibrosis.

AR antagonist 10 (Compound Y5) is a potent, orally active androgen receptor (AR) antagonist with an IC50 value of 0.04 μM. It demonstrates a dual mechanism of action: antagonizing AR by disrupting AR dimerization and inducing AR degradation through the ubiquitin-proteasome pathway. This compound shows excellent activity against various resistant AR mutants and effectively inhibits the growth of LNCaP xenograft tumors. AR antagonist 10 is applicable for research in resistant prostate cancer.

ATXN1-MED15 PPI-IN-1 is an inhibitor of the ATXN1/MED15 interaction. It binds to residues 99 to 163 of ATXN1, disrupting the interaction between ATXN1 and MED15, as well as the dimerization of polyQ-expanded ATXN1. This compound is applicable for research related to Spinocerebellar Ataxia Type 1.

8-Br-7-CH-cADPR disodium (7-Deaza-8-bromo-cADPR) is a potent antagonist of cADPR. It partially inhibits calcium increase induced by sTIR dimerization and significantly reduces axonal degeneration induced by paclitaxel.