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Catalog No.
Product Name
Application
Product Information
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Glucosylceramide Synthase Inhibitor
Lucerastat is a potent inhibitor of glucosylceramide synthase (GCS), specifically in its galactose form derived from Miglustat. This compound exhibits significant biological activity in modulating glycosphingolipid metabolism and has potential applications in the investigation of Fabry disease. Researchers may employ Lucerastat to explore therapeutic avenues and understand the pathophysiology associated with GCS-related disorders. -
GCS/GBA2 Inhibitor
Sinbaglustat is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). This N-alkyl iminosugar is orally bioavailable and capable of penetrating the blood-brain barrier, making it a valuable tool for investigating central neurodegenerative disorders linked to lysosomal dysfunction. Its unique properties facilitate research into potential therapeutic strategies for conditions such as Gaucher disease and other lysosomal storage disorders. -
Glucosylceramide Synthase Inhibitor
Ibiglustat (L-Malic acid) is a potent inhibitor of glucosylceramide synthase (GCS), demonstrating oral bioavailability and the ability to penetrate the blood-brain barrier. This compound is instrumental for research into various lysosomal storage disorders, including Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its selective inhibition of GCS makes it a valuable tool for studying the biochemical pathways associated with these conditions. -
GCS Inhibitor
TP-060 is a glucosylceramide synthase (GCS) inhibitor, exhibiting potent inhibitory activity with IC50 values of 31 nM for human GCS and 51 nM for mouse GCS. This compound is orally active and capable of penetrating the blood-brain barrier, making it a valuable tool for investigating GCS-related pathways. TP-060 is particularly relevant for research into Gaucher's disease and other conditions associated with GCS dysregulation. -
GCS Inhibitor
D-threo-PDMP hydrochloride is a potent inhibitor of glucoceramide synthase (GCS), effectively reducing glycosphingolipids such as GM3 and GD3 on the cell surface. This compound impairs glycosylation processes, leading to reduced axonal growth and branching, as well as decreased adhesion of B16 melanoma cells, effectively mimicking the effects of hyperglycemia and TGF-β1. Additionally, D-threo-PDMP hydrochloride protects hepatocytes from TNF-α-induced apoptosis by inhibiting GD3 synthesis. This reagent is valuable for research into diseases associated with glycosphingolipid metabolism. -
Glucosylceramide Synthase Inhibitor
Ibiglustat succinate is a potent glucosylceramide synthase (GCS) inhibitor with oral bioavailability and the ability to penetrate the blood-brain barrier. This compound is primarily used in research focused on Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its inhibitory action on GCS has potential implications for understanding and treating these neurodegenerative and lysosomal storage disorders. -
GCS Inhibitor
Glucosylceramide synthase-IN-2 is a potent, orally bioavailable inhibitor of glucosylceramide synthase (GCS), demonstrating IC50 values of 15 nM for human GCS and 190 nM for mouse GCS. This compound functions as a noncompetitive inhibitor in the presence of C8-ceramide and UDP-glucose. Glucosylceramide synthase-IN-2 is particularly useful for research into Gaucher's disease, offering valuable insights into the modulation of glycosphingolipid metabolism. -
GlcCer Synthase Inhibitor
D-threo-PPMP hydrochloride is a potent inhibitor of glucosylceramide (GlcCer) synthase, effectively disrupting the synthesis of glucosylceramide. This compound has been shown to block karyokinesis and reduce cyst production, making it a valuable tool for studying lipid metabolism and related pathophysiological conditions. Its application extends to research on lysosomal storage disorders and other diseases associated with glycolipid accumulation. -
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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
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. -
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. -
Aβ Inhibitor
Aβ aggregation-IN-1 is a selective inhibitor of amyloid-beta aggregation, effectively targeting the fibrillogenesis process. It demonstrates significant biological activity with IC50 values of 3.92 µM for aggregation and 7.19 µM for disaggregation. Additionally, Aβ aggregation-IN-1 inhibits malondialdehyde formation, enhances intracellular reduced glutathione levels, and reduces caspase 3 activity in neuronal cells. This compound is valuable for research in Alzheimer's disease and related neurodegenerative disorders. -
AChE Inhibitor
Buntanetap L-Tartrate is a selective acetylcholinesterase (AChE) inhibitor with an IC50 of 22.2 nM. This compound functions as a neurotoxic protein translation inhibitor, targeting proteins such as amyloid precursor protein (APP), α-synuclein (αSYN), and huntingtin protein (HTT). By obstructing the mRNA translation of β-amyloid precursor protein, Buntanetap reduces its production and exhibits anti-inflammatory properties. Its applications include research related to Alzheimer's disease and Parkinson's disease. -
β-Amyloid Inhibitor
RI-OR2-TAT is a potent inhibitor of β-Amyloid oligomerization, enhanced by the incorporation of the HIV protein transduction domain TAT. This compound exhibits a binding affinity to Aβ42 fibrils with a Kd value ranging from 58 to 125 nM. RI-OR2-TAT effectively reduces Aβ aggregation and plaque formation, mitigates microglial activation and oxidative stress, and promotes neurogenesis by increasing the proliferation of young neurons in the dentate gyrus. It is a valuable tool for research focused on neurodegenerative diseases, particularly Alzheimer's disease. -
Aβ1-40 Aggregation Inhibitor
QR-0217 is a potent inhibitor of Aβ1-40 aggregation, exhibiting an IC50 value of 7.5 µM. This compound also demonstrates the ability to inhibit α-synuclein aggregation, making it useful in studies related to neurodegenerative diseases. Additionally, QR-0217 has been shown to mitigate memory impairments associated with Aβ neurotoxicity, providing a valuable tool for research on Alzheimer's disease and related conditions. -
β-amyloid Aggregation Inhibitor
Methyl tridecanoate is a β-amyloid aggregation inhibitor that demonstrates a moderate capacity to impede the formation of β-amyloid fibrils, which are implicated in neurodegenerative diseases such as Alzheimer's. Additionally, this compound displays weak inhibition of acetylcholinesterase (AChE), an enzyme involved in cholinergic neurotransmission. Its dual activity suggests potential applications in research focused on Alzheimer's pathology and related cognitive disorders. -
Amyloid-β Inhibitor
2-Hydroxy-5-(phenyldiazenyl)benzoic acid-d5 is a deuterated derivative of 2-Hydroxy-5-(phenyldiazenyl)benzoic acid that primarily targets amyloid-β. This compound exhibits significant inhibitory activity against amyloid-β aggregation, making it valuable for research related to Alzheimer's disease and other neurodegenerative disorders. It serves as a useful tool for investigating the mechanisms of amyloid pathology and potential therapeutic strategies. -
Aβ1–42 Aggregation Inhibitor
Aβ1–42 aggregation inhibitor 2 is a potent inhibitor of Aβ1-42 aggregation, which is significant in the study of Alzheimer's disease. This compound demonstrates strong antioxidant properties, effectively chelates metal ions, and alleviates oxidative stress. Additionally, it exhibits neuroprotective and anti-neuroinflammatory activities, making it a valuable tool for research focused on neurodegenerative disorders and potential therapeutic interventions.
