pathology

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation. This product is also available as a premixed diet version (C2005 PLX5622 in AIN-76A Diet (1200 ppm)), eliminating the need for self-preparation and offering superior stability and reproducibility.

PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

CA77.1(CA) is a novel chaperon-mediated autophagy (CMA) activator for the treatment of Alzheimer's disease (AD).

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology. The activity of GsMTx4 is independent of its stereochemistry; both D-GsMTx4 and L-GsMTx4 exhibit equivalent activity in blocking the mechanosensitive current of Piezo1.

alphaSYN-IN-NAB2, a neuron-protective agent, is a protein encoded by the NAB2 gene. NAB2 effectively and selectively protects a variety of cells from alpha-SYN toxicity. NAB2 promotes endosomal transport dependent on E3 ubiquitin ligase Rsp5/Nedd4. NAB2 identifies a viable molecular node in alpha-SYN biology that corrects multiple aspects of its underlying pathology, including dysfunctional endosomes and endoplasmic reticulum to Golgi vesicles transport. NAB2 is involved in cellular processes such as cell differentiation, apoptosis and stress response, and can be used to study cancer, neurodevelopment and neuronal activity.

N-Ethyl-o-toluidine is a drug with genotoxicity and anticancer potential, exhibiting >70% growth inhibition against yeast strains with specific genetic alterations. It can also serve as an intermediate in dye synthesis.

ATN-161 acetate, a pentapeptide compound derived from the synergistic region of fibronectin, is a non-competitive integrin-alpha5 antagonist with antitumor activity that attenuates the pathology of caerulein-induced acute pancreatitis.

PLX5622 hemifumarate is a highly selective, blood-brain barrier-permeable, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and a Ki of 5.9 nM. It can be used to eliminate proliferating and specific microglia before and during disease progression and is applicable for inducing Alzheimer's disease models.

Compound STOCK1N-76816 is a reagent used in the field of biochemistry and can be applied in cross-disciplinary fields such as cell biology and molecular pathology.

Endothelin 1 (swine, human) is a potent endogenous vasoconstrictor peptide released primarily by endothelial cells and acting through ETA and ETB receptors. Endothelin 1 (swine, human) mediates vascular smooth-muscle contraction, promotes fibrosis, stimulates reactive oxygen species production, and induces pro-inflammatory signaling, making it central to studies of vascular dysfunction, hypertension, and oxidative stress–associated pathology.

Glutathione monoethyl ester, a derivative of glutathione, can protect motor neuron cells (NSC-34) from TDP-43 pathology caused by mutations, which includes reducing aggregate formation, nuclear clearance, reactive oxygen species (ROS) production, and cell death.

Antibacterialagent 266 (Compound C5) is an inhibitor of plant pathogenic bacteria that disrupts the integrity of bacterial cell membranes. It exhibits an EC50 of 24.1 μg/mL against Xanthomonasoryzaepvoryzae (Xoo) and 39.0 μg/mL against X. axonopodispvcitri (Xac). Antibacterialagent 266 is valuable for research in plant pathology and the development of agricultural antibacterial agents.

BF-170 is a selective tau fiber-binding agent with an EC50 of 221 nM. It demonstrates excellent blood-brain barrier penetration, reaching a concentration of 9.1% ID/g in brain tissue 2 minutes after intravenous injection in mice (with a clearance rate of 0.25% ID/g at 30 minutes). BF-170 can serve as a probe for imaging tau protein pathology in Alzheimer's disease (AD). It plays a significant role in early-stage Alzheimer's disease studies and holds promise for imaging research in tau-related neurodegenerative diseases.

VEN-02XX is an orally active NLRP3 inhibitor capable of penetrating the brain. It effectively suppresses the release of IL-1β and IL-18, with IC50 values of 0.3 and 0.28 μM, respectively. In the 5XFAD/Rubicon KO mouse model, VEN-02XX aids in restoring memory and cognition, inhibits microgliosis, and alleviates neuroinflammation and tau protein pathology. This compound is valuable for Alzheimer's disease (AD) research.

MRL828 is a compound that combines a Tau pathology-binding ligand with a guanine group modified by ATTEC technology, allowing it to selectively target aggregated tau proteins for clearance via the autophagy-lysosome pathway (ALP). MRL828 reduces intracellular Tau aggregates and facilitates the secretion of Tau.

20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.

γ-[(6-Aminohexyl)-imido]-ATP-biotin is a versatile dye. Such dyes are vital tools in biological experiments, aiding researchers in observing and analyzing cell structures, tracking biomolecules, evaluating cell functionality, distinguishing cell types, detecting biomolecules, studying tissue pathology, and monitoring microorganisms. Their applications range widely from foundational science research to clinical diagnostics. Additionally, dyes are extensively used in traditional fields like textile dyeing and emerging sectors such as functional textile processing, food colorants, and dye-sensitized solar cells.

SGC-NSP2hel-1 (RA-0188293) is a potent and selective oral inhibitor of the nsP2 helicase, with a CC50 greater than 250 µM and a selectivity index over 4000. It exhibits broad-spectrum activity against various alphaviruses. In preclinical small animal models of chikungunya virus (CHIKV) disease, SGC-NSP2hel-1 reduces viral replication and limits virus-induced pathology by forming a stable complex with nsP2 and ATP.

SRI-22136 is a Delta opioid receptor (DOR) antagonist that can cross the blood-brain barrier with an IC50 of 0.42 nM. It lacks agonistic activity on DOR, MOR, and KOR, functioning solely as an antagonist with IC50 values of 370 nM for MOR and 54 nM for KOR, thereby avoiding addiction/aversion effects. SRI-22136 effectively inhibits DADLE (a DOR agonist)-induced BACE1 activity with an IC50 of 120 nM. It can completely prevent Alzheimer’s disease-like pathology in mouse models and is applicable for Alzheimer's research.

Lithium salicylate (Salicylic acid lithium) is an orally bioavailable lithium salt. It reduces tau protein phosphorylation and alleviates related pathology in Alzheimer's disease mouse models. Lithium salicylate (Salicylic acid lithium) is utilized in Alzheimer's disease research.

ACI-19278 is a TDP-43 PET tracer with an average Kd of 25 nM. It selectively binds to pathological TDP-43 aggregates without cross-reactivity to proteins such as Aβ and Tau. Using positron emission tomography ([18F]ACI-19278), this compound has successfully visualized TDP-43 pathology in the human brain. ACI-19278 is suitable for in vivo diagnostic research of TDP-43 protein pathologies.

INVA8001 is a highly selective and orally active chymase inhibitor, with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell protease 4 (mMCP-4). It exhibits IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, demonstrating over 1000-fold selectivity against other related serine proteases. In a mouse model of primary sclerosing cholangitis (PSC), INVA8001 inhibits mast cell activity, improves biliary pathology, alleviates cholestasis, and displays anti-inflammatory and anti-fibrotic properties.

(E),(Z)-RNF5 agonist 1 (Compound Analog-1) is an RNF5 agonist that enhances the ubiquitin-mediated degradation of the SARS-CoV-2 E protein. It effectively inhibits SARS-CoV-2 replication and significantly reduces lung pathology and systemic inflammation in mouse infection models. Additionally, (E),(Z)-RNF5 agonist 1 exhibits potent cytotoxicity against neuroblastoma and melanoma cells. This compound is relevant for cancer and antiviral research.