oligomerization

VBIT-4 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 17 μM). VBIT-4 can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).

NLRP3 AIM2-IN-3 is a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation in a species-specific manner. It has an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3 AIM2-IN-3 is a potent inhibitor of NLRP3 and AIM2 inflammasome-dependent cell lysis with an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3 AIM2-IN-3 inhibits LPS nigericin NLRP3 AIM2-IN-3 inhibits LPS nigericin-stimulated cell lysis in THP-1 macrophages with an IC50 value of 0.077 ± 0.008 μM. NLRP3 AIM2-IN-3 interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC, inhibiting oligomerization of ASC.

Bis-T-23 is a promoter of actin-dependent dynamin oligomerization, an HIV-I integrase inhibitor, and a Telstar derivative. Bis-T-23 promotes actin-dependent dynamin oligomerization. Bis-T-23 can be used in studies of HIV and chronic kidney disease (CKD).

G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) agonist that promotes glucose-6-phosphate dehydrogenase (G6PD) oligomerization to a catalytically competent form. G6PD activator AG1 reduces oxidative stress in cells and zebrafish, reduces chloroquine or diamide-induced oxidative stress in human erythrocytes, and can be used to study glucose-6-phosphate dehydrogenase deficiency.

3,6-DMAD dihydrochloride is an acridine derivative and a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride can induce IL-6 secretion by exploiting the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride is a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride has inhibitory effects on IRE1α oligomerization and RNase activity. 3,6-DMAD dihydrochloride can be used in cancer research.

WJ-39 is an orally active aldose reductase (AR) inhibitor that ameliorates renal lesions in diabetic nephropathy through activation of Nrf2 signaling, and may be used to ameliorate renal insufficiency and fibrosis.WJ-39 inhibits oxidative stress and inhibits the activation of the inflammatory vesicle of the oligomerization structural domain-like receptor family, pyrin structural domain 3 (NLRP3).

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM).

MSN-50, an inhibitor of Bax and Bak oligomerization, inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection.

hAChE-IN-1 (Compound 24) is a potent inhibitor of human acetylcholinesterase (hAChE), with an inhibition concentration half-maximum (IC50) of 1.09 μM, and inhibits tau-oligomerization with an effective concentration half-maximum (EC50) of 2.71 μM as determined by a cellular tau fluorescence resonance energy transfer (FRET) assay [1].

NLRP3-IN-21 (compound L38) is an inhibitor of the NLRP3 inflammasome with anti-inflammatory properties, suppressing inflammasome activation and pyroptosis by inhibiting gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly [1].

NOD1 2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1 2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1 2) of 67.6 minutes. Additionally, NOD1 2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

CBR-5884 is an selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH

FK-565 is a ligand of nucleotide-binding oligomerization domain-1 (NOD1) that induces a mouse model of arteritis.

NOD-IN-1 (Compound 4) is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors.

RI-OR2-TAT is a brain-penetrable inhibitor targeting β-amyloid (β-Amyloid) oligomerization. It is engineered by integrating the HIV protein transduction domain TAT into RI-OR2. RI-OR2-TAT binds to Aβ42 fibrils with a Kd value of 58-125 nM. It reduces Aβ aggregation and plaque levels, diminishes microglial activation and oxidative damage, and enhances the number of young neurons in the dentate gyrus.

CBI1 formic is a covalent inhibitor of BAX, selectively derivatizing BAX at C126 and inhibiting its activation by triggering with a ligand or point mutation. This compound effectively blocks the t-2-hex lipidation and oligomerization of BAX. Additionally, CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutations, or t-2-hex.

AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 protects against mitochondrial dysfunction[1]. AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis.

VBIT-3 is a voltage-dependent anion channel 1 (VDAC1) oligomerization inhibitor (Kd: 31.3 μM). VBIT-3 also is an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders (such as neurodegenerative and cardiovascular diseases).

Tau-0N4R-IN-1 (Compound 6T) is a brain-penetrant inhibitor of tau0N4R oligomerization. It effectively inhibits the fibrillization of tau 0N4R, 2N3R, and 2N4R, showcasing potent anti-seeding effects against tau in vitro, and can dose-dependently reduce α-syn oligomerization while preventing the formation of α-syn inclusions. Tau-0N4R-IN-1 demonstrates stability in mouse microsomes and reduces Aβ plaques derived from the brain tissue of AD patients. Moreover, it exhibits favorable pharmacokinetic properties in mice.

YOK-1304, an autophagy-targeting chimera (AUTOTAC), induces self-oligomerization of p62.

Entacapone sodium salt inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.Entacapone sodium salt is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.

MSN-125 effectively inhibits Bax Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond

NSC145366 is an inhibitor of Hsp90 activities which targets the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation. NSC145366 increases Hsp90 oligomerization resulting in allosteric inhibition of NTD ATPase activity (IC50=119μM) but does not compete with NTD or CTD-ATP binding.

tau Protein α-synuclein-IN-2 (Compound 14T) is a tau and α-synuclein inhibitor capable of crossing the blood-brain barrier. It reduces α-synuclein oligomerization in a dose-dependent manner through a thiourea linker structure. In biosensor cells, tau Protein α-synuclein-IN-2 prevents tau aggregation seed effects. In the M17D neuroblastoma model, this compound exhibits anti-inclusion effects and reduces Aβ plaque formation. tau Protein α-synuclein-IN-2 shows potential for Alzheimer's and Parkinson's disease research.