disruptor

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.

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.

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

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.

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.

AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).

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.

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.

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

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

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.

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

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

KG-548 is an ARNT TACC3 disruptor and HIF-1α inhibitor. It competitively binds the ARNT PAS-B domain with TACC3, directly interfering with the formation of the ARNT TACC3 complex. ARNT, also known as HIF-β, stands for aryl hydrocarbon receptor nuclear translocator [1][2].

Dipentyl phthalate-3,4,5,6-d4 is a deuterated compound of Dipentyl phthalate. Dipentyl phthalate has a CAS number of 131-18-0. Diamyl phthalate is an agent of endocrine disruptor.

AKAP disruptor. Selectively binds PKA-RI with high affinity (KD values are 6.2 and 12.1 nM for the RIα and β subunits, respectively) and blocks its interaction with AKAP. Inhibits type I PKA-mediated phosphorylation in live cells. Cell permeable.

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.

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)

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].

Diamyl phthalate is an agent of endocrine disruptor.

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.

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.