Catalog No.
Product Name
Application
Product Information
Citations
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GCS Inhibitor
Glucosylceramide synthase-IN-3 is a potent inhibitor of glucosylceramide synthase (GCS), demonstrating an IC50 of 16 nM for human GCS. This compound is brain-penetrant and orally active, making it suitable for in vivo studies. Glucosylceramide synthase-IN-3 is primarily used in research focused on Gaucher's disease and related glycosphingolipid metabolism disorders. -
Rate-limiting Enzyme
Alpha-1,2-Fucosyltransferase (α1,2FucT) is a rate-limiting enzyme that catalyzes the synthesis of the Lewis y carbohydrate antigen, which is predominantly found on cell membranes. This enzyme plays a crucial role in the glycosylation processes relevant to cancer biology and cell adhesion mechanisms. α1,2FucT is utilized in biochemical studies to investigate its impact on tumor progression, cellular interactions, and the formation of cancer-associated carbohydrate antigens. -
GlcCer Synthase Inhibitor
D-threo-PPMP is a potent inhibitor of glucosylceramide (GlcCer) synthase, a critical enzyme in sphingolipid metabolism. Inhibition of GlcCer synthase by D-threo-PPMP has been shown to block karyokinesis and decrease cyst production, making it valuable for research into lysosomal storage disorders and related pathologies. This compound is essential for studies aimed at elucidating the role of GlcCer in cellular processes and disease mechanisms. -
Glucosylceramide Synthase Inhibitor
Ibiglustat hydrochloride is a potent glucosylceramide synthase (GCS) inhibitor that effectively penetrates the blood-brain barrier. This compound is primarily used in research related to Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its mechanism of action contributes to the modulation of glucocerebroside metabolism, offering a valuable tool for studies focused on lysosomal storage disorders and related neurodegenerative conditions. -
Erythro Isomer of PDMP
D,L-erythro-PDMP is the erythro isomer of PDMP and acts as an inhibitor of UDP-glucose:ceramide glucosyltransferase. This compound exhibits significant growth inhibition of cultured rabbit skin fibroblasts, making it a valuable tool for studying glycosphingolipid metabolism and its effects on cell proliferation. D,L-erythro-PDMP is useful in research applications focused on lipid biology and associated diseases. -
Glucosylceramide Synthase Inhibitor
(−)-L-threo-PDMP hydrochloride is a potent inhibitor of glucosylceramide synthase (GCS). This compound has been shown to promote the proliferation of cultured aortic smooth muscle cells and elevate levels of lactosylceramide (LacCer) in B16 melanoma cells. Its unique activity profile makes it a valuable tool for research applications related to glycosphingolipid metabolism and cellular signaling pathways. -
GCS Inhibitor
EXEL-0346 is a potent glucosylceramide synthase (GCS) inhibitor, demonstrating an IC50 value of 2 nM. This compound enhances insulin signaling through an increase in pAkt levels while effectively decreasing the concentrations of glucosylceramide, lactosylceramide, and GM3. EXEL-0346 shows promise in addressing metabolic disorders, particularly obesity and diabetes, making it a valuable tool for research in these areas. -
GCS Inhibitor
Glucosylceramide synthase-IN-4 is a potent inhibitor of glucosylceramide synthase (GCS), exhibiting an IC50 value of 6.8 nM. This compound demonstrates favorable pharmacokinetic properties and stability in human hepatocytes, making it suitable for in vitro studies. Additionally, Glucosylceramide synthase-IN-4 exhibits effective central nervous system (CNS) penetration and maintains acceptable selectivity for PXR, facilitating research into GCS-related pathways and potential therapeutic applications in metabolic disorders. -
FUT8 Inhibitor
FUT8-IN-1 is a potent inhibitor of α-1,6-fucosyltransferase (FUT8), exhibiting a KD of 49 nM and an IC50 of approximately 50 µM. This compound generates a highly reactive naphthoquinone imine intermediate upon interaction with FUT8, effectively inhibiting its enzymatic activity. FUT8-IN-1 is valuable for investigating the role of FUT8 in glycosylation processes and its implications in various biological research applications. -
AAK1 Inhibitor
BMS-986176 is a potent and selective inhibitor of adaptor associated kinase 1 (AAK1) with an IC50 value of 2 nM. This compound is designed for effective brain penetration, making it a valuable tool in the investigation of neurodegenerative diseases. It is applicable in research focused on the modulation of AAK1 pathways and their implications in various neurological disorders. -
AAK1 Inhibitor
AAK1-IN-12 is a selective inhibitor of the AP2-associated kinase 1 (AAK1) that demonstrates oral bioavailability and the ability to cross the blood-brain barrier. This compound has important implications for research into neurodegenerative disorders, including schizophrenia, Parkinson's disease, neuropathic pain, and Alzheimer's disease. AAK1-IN-12 serves as a valuable tool for investigating the therapeutic potential of AAK1 modulation in various neurological contexts. -
AAK1 Inhibitor
LP-922761 is a selective inhibitor of adapter protein-2 associated kinase 1 (AAK1), demonstrating potent activity with IC50 values of 4.8 nM in enzyme assays and 7.6 nM in cellular assays. Additionally, LP-922761 inhibits BMP-2-inducible protein kinase (BIKE) at an IC50 of 24 nM. Importantly, it shows no significant activity against cyclin G-associated kinase (GAK), opioid receptors, adrenergic α2 receptors, or GABAa receptors, making it a valuable tool for studying AAK1-related signaling pathways and its role in cellular processes. -
AAK1
BMS-911172 is an inhibitor of adaptor-associated kinase 1 (AAK1), exhibiting an IC50 value of 35 nM. This compound is primarily used in research focused on modulating clathrin-mediated endocytosis and exploring the role of AAK1 in cellular processes. Its ability to selectively inhibit AAK1 makes it a valuable tool for investigating signaling pathways related to receptor internalization and trafficking. -
AAK1 Inhibitor
BMT-124110 is a highly selective inhibitor of AAK1 (AP2-associated protein kinase 1) with an IC50 value of 0.9 nM. This compound exhibits notable antinociceptive activity, making it relevant in pain management research. Additionally, BMT-124110 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 17 nM and 99 nM, respectively, further supporting its utility in kinase-related studies. -
AAK1 Inhibitor
SGC-AAK1-1N is a selective inhibitor of AAK1 (AP2 associated kinase 1) with an IC50 value of 1.8 μM. This compound is utilized in research to elucidate the role of AAK1 in cellular processes, particularly in clathrin-mediated endocytosis and signaling pathways. Its potency makes it a valuable tool in studies focused on understanding the therapeutic potential of AAK1 modulation in various diseases. -
AAK1 Inhibitor
BMS-901715 is a highly selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM. This compound disrupts clathrin-mediated endocytosis, making it valuable for studying cellular processes related to membrane trafficking. BMS-901715 is particularly useful in research applications focused on viral infections and the modulation of synaptic transmission. -
AAK1 Inhibitor
AAK1-IN-2 TFA is a selective and potent inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), demonstrating an IC50 value of 5.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research in neuropathic pain mechanisms. AAK1-IN-2 TFA enables the investigation of AAK1's role in various neurological conditions, providing insights into potential therapeutic targets for pain management. -
AAK1 Inhibitor
AAK1-IN-3 is a potent inhibitor of adaptor protein 2-associated kinase 1 (AAK1), exhibiting an IC50 of 11 nM. This quinoline analogue effectively penetrates the blood-brain barrier, making it suitable for investigating the role of AAK1 in neuropathic pain mechanisms. AAK1-IN-3 is a valuable tool for research focused on neuropharmacology and the modulation of pain pathways. -
AAK1 Inhibitor
AAK1-IN-4 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 4.6 nM. This orally active compound effectively penetrates the central nervous system, with a filtration Ki of 0.9 nM and a cell IC50 of 8.6 nM. AAK1-IN-4 is primarily utilized in research studies focused on neuropathic pain, offering insights into its underlying mechanisms and potential therapeutic applications. -
AAK1 Inhibitor
AAK1-IN-3 TFA is a quinoline derivative that selectively inhibits adaptor protein 2-associated kinase 1 (AAK1) with an IC50 of 11 nM. This compound demonstrates significant brain penetration and is suitable for investigating neuropathic pain mechanisms. Its ability to modulate AAK1 activity makes it a valuable tool for research applications focused on pain pathways and related neurobiological processes. -
AAK1 Inhibitor
HW161023 is a potent inhibitor of AP2-associated protein kinase 1 (AAK1), demonstrating an IC50 of 5.4 nM against AAK1 and a much higher IC50 of 11.9 μM against hERG. This compound has shown efficacy in alleviating pain in a chronic constriction injury model of the sciatic nerve in rats. HW161023 is valuable for research in pain mechanisms and the modulation of AAK1-related signaling pathways. -
AAK1 Inhibitor
AAK1-IN-10 is a selective inhibitor of adapter-associated kinase 1 (AAK1), exhibiting potent enzyme inhibitory activity with an IC50 of 9.62 nM. This compound primarily functions by impairing the activity of AAK1, a kinase involved in various cellular processes. AAK1-IN-10 demonstrates low cardiotoxicity, with an IC50 of 13.7 μM, making it a suitable candidate for research into conditions such as diabetic neuropathy and postherpetic pain. Its distinct mechanism and safety profile facilitate investigations into therapeutic applications targeting nerve pain and associated disorders. -
AAK1 Inhibitor
AAK1-IN-2 is a selective inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), exhibiting an IC50 of 5.8 nM. This compound demonstrates the ability to penetrate the blood-brain barrier, making it suitable for neurological research. AAK1-IN-2 is particularly relevant for studies investigating the mechanisms underlying neuropathic pain. -
AAK1 Inhibitor
AAK1-IN-5 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 1.2 nM and a filtrate Ki of 0.05 nM, along with a cell-based IC50 of 0.5 nM. This compound is notable for its ability to penetrate the central nervous system and is orally active, making it suitable for in vivo studies. AAK1-IN-5 is primarily used in research focused on neuropathic pain, providing a valuable tool for understanding AAK1's role in pain pathways. -
PROTAC
PROTAC AAK1 Degrader-1 is a potent PROTAC designed to selectively degrade the AAK1 protein, a known modulator of clathrin-mediated endocytosis. This compound facilitates targeted protein degradation, thereby influencing cellular pathways critical in cancer research. Its application is valuable for studying the role of AAK1 in tumor biology and therapeutic resistance, potentially leading to innovative cancer treatment strategies.
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AAK1 Inhibitor
BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1), targeting its activity to modulate cellular processes. This compound effectively inhibits the phosphorylation of the μ2 peptide by AAK1, demonstrating an IC50 value of 2.8 nM. BMT-046091 is useful in research applications studying AAK1's role in endocytic trafficking and signaling pathways, contributing to a better understanding of its implications in various diseases. -
Aβ Aggregation Inhibitor
TDI-2760 is an Aβ aggregation inhibitor with an IC50 of 1.67 μM, specifically targeting the aggregation of amyloid-beta peptides. This compound effectively inhibits Aβ-fibrinogen interactions and modulates contact system activation induced by Aβ42. TDI-2760 is suitable for research focused on Alzheimer's disease, particularly in the study of vascular abnormalities associated with Aβ aggregation. -
Buffering Agent
HEPPS is a buffering agent with an effective pH range of 7.3 to 8.7. This compound has demonstrated the ability to reduce amyloid beta (Aβ) aggregate-induced memory deficits and improve cognitive functions in murine models. HEPPS is orally active and capable of crossing the blood-brain barrier, making it valuable for neuroscience research. -
TDP-43 Binder
rTRD01 is a selective TDP-43 binder that specifically targets the RRM1 and RRM2 domains of TDP-43, partially disrupting its interaction with c9orf72 repeat RNA while preserving binding to canonical sequences. This compound demonstrates significant neuroprotective effects in zebrafish models, improving motor function and providing protection against paraquat-induced neurodegeneration without teratogenic effects at elevated concentrations. rTRD01 is a valuable tool for investigating amyotrophic lateral sclerosis and related TDP-43 proteinopathies, offering insights into the molecular mechanisms involved in these conditions. -
β-amyloid (Aβ) Binder
Pittsburgh Compound B (PiB) is a targeted β-amyloid (Aβ) binder, designed as a PET tracer for the visualization of Aβ deposition in the brain. It exhibits a high affinity for Aβ(1-40) fibrils with a Ki value of 678.4 nM. The compound can be modified using click chemistry, allowing for the development of fluorescent conjugates for applications in fluorescence imaging and ultrastructural studies. Pittsburgh Compound B is particularly relevant for research focusing on Alzheimer's disease and the characterization of Aβ complexes. -
Amyloid-β 42 Inducer
Aftin-5 is an inducer of Amyloid-β 42 (Aβ42) that functions by modulating β-secretase and γ-secretase activity, leading to an increase in Aβ42 levels while decreasing Aβ38 levels. This compound affects mitochondrial ultrastructure, which is essential for its biological activity. Aftin-5 displays moderate cytotoxicity in various cell lines, including SH-SY5Y, HT22, N2a, and N2a-AβPP695, with IC50 values ranging from 150 μM to 194 μM. Its role in research makes it a valuable tool for studying Alzheimer's disease and related neurodegenerative conditions. -
BACE1/BACE2 Inhibitor
NB-360 is a potent dual inhibitor of β-secretase 1 and 2 (BACE1/BACE2) with IC50 values of 5 nM and 6 nM, respectively. This compound is brain-penetrable and orally active, effectively inhibiting the accumulation of amyloid-β proteins. NB-360 is valuable for research in inflammation and neurological diseases, particularly Alzheimer's disease. -
APP Degrader
APP degrader-1 is an orally active compound designed to target the amyloid precursor protein (APP). It induces the degradation of APP and effectively reduces the extracellular release of Aβ42. By binding to both CAPRIN1 and APP, APP degrader-1 enhances their interaction and facilitates CAPRIN1-mediated APP degradation via the endosome-lysosome pathway. This compound holds potential for research applications related to Alzheimer's disease and protein misfolding disorders. -
β-Amyloid
β-Amyloid (1-16) is a peptide fragment derived from β-Amyloid, known for its ability to bind various metal ions. This fragment plays a significant role in the formation of amyloid plaques, which are characteristic of Alzheimer's disease pathology. Researchers can utilize β-Amyloid (1-16) to investigate metal-induced aggregation mechanisms and assess its potential contributions to neurodegenerative processes associated with Alzheimer's disease. -
Amyloid Inhibitor
4-Hydroxyindole is an amyloid inhibitor that plays a critical role in the disruption of amyloid fibrillization. This compound has been shown to induce alterations in liver function, thyroid activity, and blood glucose levels in preclinical models. Its unique properties make 4-Hydroxyindole a valuable tool for investigating neurodegenerative diseases and metabolic disorders. Researchers can leverage its potential to explore therapeutic avenues for amyloid-related pathologies. -
TDP-43 Inhibitor
ACI-19626 is a TDP-43 inhibitor that targets TDP-43 aggregation. This compound is valuable for investigating the role of TDP-43 in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Its utility in preclinical studies helps elucidate the molecular mechanisms underlying these conditions and aids in the identification of potential therapeutic strategies. -
Aβ1-42 Aggregation Inhibitor
Aβ1–42 aggregation inhibitor 1 is a potent inhibitor of Aβ1-42 aggregation, targeting its self-mediated aggregation pathway. This compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 2.64 μM and 1.29 μM, respectively. At a concentration of 25 μM, it reduces Aβ1-42 aggregation by 51.29%. Aβ1–42 aggregation inhibitor 1 is suitable for research applications focused on the mechanisms of Alzheimer's disease and potential therapeutic interventions. -
AChE Inhibitor
Phenserine is a potent, noncompetitive inhibitor of acetylcholinesterase (AChE), derived from Physostigmine. It selectively targets AChE and has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). This compound is primarily utilized in research related to cognitive function and the progression of Alzheimer's disease, demonstrating potential therapeutic benefits in enhancing cognitive performance. -
QPCTL Inhibitor
QP5038 is a specific inhibitor of the enzyme QPCTL, exhibiting an IC50 value of 3.8 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology. QP5038 can be utilized in studies focused on understanding the role of QPCTL in tumor metabolism and potential therapeutic strategies. -
PHF6/Tau Disrupter
Cl-NQTrp is a potent disrupter of preformed fibrillar aggregates associated with Tau-derived PHF6 (VQIVYK) peptides and full-length tau protein. This compound exhibits substantial activity in modulating tau aggregation, making it a valuable tool for research focused on tauopathies and Alzheimer's disease. Its role in disrupting tau pathology positions Cl-NQTrp as a key reagent for studies investigating therapeutic strategies against neurodegenerative disorders characterized by abnormal tau accumulation. -
Glutaminyl Cyclase Inhibitor
PBD-150 is a selective inhibitor of human glutaminyl cyclase (hQC), specifically targeting the Y115E-Y117E variant with a Ki value of 490 nM. This compound exhibits significant inhibitory activity, making it a valuable tool for studying the role of glutaminyl cyclase in neurodegenerative diseases. PBD-150 can be applied in research focused on pathologies associated with abnormal protein aggregation and its therapeutic potential. -
Aβ Aggregation Inhibtior
Dihydrochalcone is an Aβ aggregation inhibitor that destabilizes Aβ17-42 protofibrils by disrupting the β-sheet structure in the β1 region. This compound effectively targets both U-shaped Aβ40/Aβ42 and S-shaped Aβ42 protofibrils by binding to their respective protofibril cavities. Dihydrochalcone, primarily derived from the daemonorops draco tree, is of significant interest in Alzheimer's disease research and offers potential for studying therapeutic strategies aimed at preventing amyloid-beta aggregation. -
TFEB Activator
TFEB Activator 3 is a potent activator of TFEB, enhancing its nuclear translocation and promoting lysosome biogenesis. Demonstrated effects include a 44% increase in nuclear translocation at 10 µM after 3 hours and up to 97% at 30 µM under the same conditions. This compound is significant for research into Alzheimer’s disease, as it effectively crosses the blood-brain barrier, making it a valuable tool for studies on neurodegeneration and cellular clearance mechanisms. -
Bexarotene Derivative
OAB-14 is a derivative of Bexarotene that enhances the clearance of β-amyloid in APP/PS1 transgenic mice, addressing Alzheimer's disease-related pathologies and cognitive deficits. This compound demonstrates the ability to improve the functionality of the endosomal-autophagic-lysosomal pathway, making it a valuable tool for research into Alzheimer's disease mechanisms and potential therapeutic interventions. -
Amyloid-β Inhibitor
D-KLVFFA is a potent inhibitor of Amyloid-β assembly, exhibiting an IC50 value of 2.6 μM. This peptide is utilized in research focused on Alzheimer's disease, providing insights into the mechanisms of amyloid plaque formation and potential therapeutic interventions. Its application can contribute to the understanding of neurodegenerative processes and the development of Alzheimer’s disease treatments. -
Antioxidant Agent
Crocetin monomethyl ester serves as an antioxidant agent, derived from Crocus sativus. It exhibits significant anti-inflammatory and neuroprotective properties, making it valuable in neurological research. This compound promotes the clearance of amyloid-β by inducing autophagy through the STK11/LKB1-mediated AMPK pathway, highlighting its potential application in Alzheimer’s disease studies and related neurodegenerative disorders. -
Amyloid-Beta and Tau Inhibitor
Aβ/tau aggregation-IN-1 is a selective inhibitor of amyloid-beta (Aβ1-42) β-sheet formation and tau protein aggregation. With KD values of 160 μM for Aβ1-42 and 337 μM for tau, this compound demonstrates significant potential in research related to neurodegenerative disorders such as Alzheimer's disease. Its ability to cross the blood-brain barrier further supports its use in studies aimed at understanding the pathophysiology of amyloid and tau accumulation in the central nervous system. -
Aβ/tau Protein Aggregation Inhibitor
DN5355 is a small molecule inhibitor of amyloid β protein (Aβ) and hyperphosphorylated tau protein aggregation. It effectively inhibits the formation of Aβ and tau fibrils while also promoting the disaggregation of pre-formed aggregates. This compound is valuable for research applications focused on Alzheimer's disease and the underlying mechanisms of protein aggregation associated with neurodegeneration. -
Aβ40 Aggregation Inhibitor
Biphenyl-3′,3,4,4′-tetrol (BPT) is a potent inhibitor of Aβ40 aggregation, targeting the aggregation process associated with amyloid-beta peptides. This compound is relevant for research into neurodegenerative diseases, particularly Alzheimer's disease, by facilitating studies aimed at understanding and potentially mitigating the pathological effects of amyloid plaque formation. -
Amyloid-β Inhibitor
Semilicoisoflavone B is an isoflavone derived from Glycyrrhiza uralensis Fisch, functioning primarily as an inhibitor of amyloid-β (Aβ) secretion. It reduces Aβ levels by inhibiting the expression and activity of β-secretase-1 (BACE1). This compound enhances PPARγ expression while simultaneously inhibiting STAT3 phosphorylation, leading to decreased BACE1 levels. Semilicoisoflavone B is relevant for research into Alzheimer's disease and mechanisms of neurodegeneration.
