disruptor

OSIP-486823(CP248) is a novel and potent microtubule disruptor with affinity for both protein kinase G (PKG) and microtubules.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

Avobenzone is a dibenzoylmethane endocrine disruptor that binds directly to estrogen receptor β, acting as an estrogen agonist. It is one of the most widely used filters in sunscreens for photoprotection of skin in the UV band.

Bisphenol A is an endogenous metabolic compound of phenols and is widely used in the production of epoxy resins and polycarbonate plastics. It is reproductive, developmental and systemic toxicant and is often classified as an endocrine disruptor. It has been linked to many diseases, including respiratory disease, cardiovascular disease, diabetes, kidney disease, obesity and reproductive disorders.

Atrazine (Oleogesaprim) is an herbicide that does not occur naturally,and is a selective triazine herbicide. Atrazine (Oleogesaprim) is also a potent endocrine disruptor.

4-N-Nonyloxyphenol (4-nonoxyphenol), a heterogeneous photosensitizer based on kaolinite nanotubes, is a widely used pesticide and endocrine disruptor for the photodegradation of phenol-based pesticides.

Butylhydroxyanisole (BHA) is an antioxidant consisting of a mixture of two isomeric organic compounds, 2-tert-butyl-4-hydroxyanisole and 3-tert-butyl-4-hydroxyanisole.

Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor (IC50: 140 nM) that inhibits cell migration and reverses drug resistance.

Equilenin (E 400), a natural estrogen, is a specific fluorescent probe for steroid-protein interactions in sex steroid-binding proteins and has a high binding affinity for sex steroid-binding proteins (SBPs) Equilenin is an endocrine disruptor and can be used in the study of breast cancer.

4-Octylphenol is an endocrine disruptor with gender-specific effects on male germ cells, significantly reducing the mitotic index and the number of spermatogonia. It also causes inflammatory damage in the gills of carp by activating the complement system through the C3a C3a receptor (C3a C3aR) axis and C5a C5a receptor 1 (C5a C5aR1) axis. Furthermore, 4-Octylphenol induces immune suppression by disrupting the balance between helper T (Th) cells 1 Th2 and regulatory T (Treg) Th17 cells, and triggers inflammatory damage through the Toll-like receptor 7 (Toll-like Receptor (TLR)) inhibitor κBα nuclear factor κB (TLR7 IκBα NF-κB) pathway.

Diamyl phthalate is an agent of endocrine disruptor.

MDG506 is a novel selective androgen receptor (AR) interaction disruptor that demonstrates low cytotoxicity in prostate cancer (PCa) models and shows a dose-dependent reduction in prostate-specific antigen expression induced by classical antiandrogens.

ELR510444 (LR510444) is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.

STAD-2 is a cell permeable akap disruptor, selectively binding to pka-rii and blocking the interaction of pka-ri with akap

THIQ-20c is a steroidomimetic and chimeric microtubule disruptor.

CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020)

4-tert-Octylphenol diethoxylate is a degradation product of the multi-purpose surfactant, Triton X. A known environmental contaminant, 4-tert-octylphenol diethoxylate is reported to be an endocrine disruptor in animal and human research studies, producing weak estrogenic effects.

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

M-COPA is a golgi disruptor which inhibits cell surface expression of MET protein and the ADP-ribosylation factor 1 (Arf1) activation. M-COPA also inhibits angiogenesis through suppression of both VEGFR1 2 and nuclear factor-kappaB (NF-kappaB) signaling pathways.

WL47 TFA is a selective small molecule caveolin-1 oligomer disruptor that disrupts CAV1 oligomers.

Microtubule Inhibitor 8 (MP-HJ-1b) serves as a potent disruptor of microtubule function, inducing cell death via ferroptosis and demonstrating anti-tumor effects [1] [2].

NY2267 (Acetic acid, 2-[[6-[2-(cyclohexylamino)-1-[[(4-methoxyphenyl)methyl](2-pyridinylcarbonyl)amino]-2-oxoethyl]-2-naphthalenyl]oxy]-, 1,1-dimethylethyl ester) is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM.

Kea1-97 is a selective disruptor of interaction between thioredoxin and caspase-3 (IC50 = 10 μ M). Kea1-97 destroys the interaction between thioredoxin and caspase 3 and activates caspases without affecting the activity of thioredoxin.

Indusatumab vedotin (MLN-0264; AKT-264) is an antibody-drug conjugate (ADC) that combines a human anti-guanylate cyclase C (GCC) antibody with the microtubule-disruptor monomethyl auristatin E, demonstrating anti-proliferative effects on pancreatic cancer cell lines by arresting the cell cycle at the G2 M phase and inducing apoptosis [1].