Catalog No.
Product Name
Application
Product Information
Citations
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β-catenin:TCF Interaction Inhibitor
β-Catenin inhibitory peptoid targets the β-catenin:TCF interaction, exhibiting an IC50 of 5.44 µM. This compound effectively inhibits Wnt signaling with an IC50 of 0.105 µM and androgen receptor signaling with an IC50 of 1.02 µM in prostate cancer cell lines. The peptoid significantly reduces cell proliferation, making it a valuable tool for research in cancer biology and therapeutic development. -
Wnt/β-catenin Inhibitor
Wnt/β-catenin-IN-3 is a potent inhibitor of the Wnt/β-catenin signaling pathway, demonstrating low micromolar GI50 values across various cancer cell lines. This compound induces G2/M cell cycle arrest by activating the p53-p21 pathway and promotes apoptotic cell death through both intrinsic and extrinsic mechanisms in colon cancer cells. It serves as a valuable tool for investigating the role of Wnt/β-catenin signaling in cancer biology and therapeutic applications. -
β-catenin Inhibtior
β-catenin-IN-8 is a potent inhibitor of β-catenin, targeting the Wnt signaling pathway. This compound effectively reduces the levels of β-catenin and c-Myc proteins, leading to downregulation of Wnt-target genes such as Fgf20 and Sall4. β-catenin-IN-8 exhibits anti-cancer activity in colorectal cancer models and demonstrates favorable metabolic stability, making it a valuable tool for research into cancer biology and therapeutic strategies. -
Wnt/β-catenin Inhibitor
Getacatetide is a peptide-based inhibitor of the Wnt/β-catenin signaling pathway. This compound is designed to interfere with the activation of Wnt target genes, making it a valuable tool for investigating the role of Wnt/β-catenin signaling in solid tumors. Getacatetide's ability to disrupt this pathway facilitates research into cancer biology and the development of potential therapeutic strategies. -
Wnt Inhibitor
Halofenate acts as a Wnt inhibitor, impacting the Wnt signaling pathway crucial for cell proliferation and differentiation. It demonstrates significant biological activity by effectively reducing serum triglyceride levels by 50% in hypertriglyceridemic patients and decreasing serum uric acid by 30%, highlighting its potential uricosuric effects. Halofenate additionally increases plasma thyroxine (T4) levels, suggesting implications for thyroid function regulation, supported by in vitro studies showing its ability to displace T4 from thyroid-binding proteins. This compound can be valuable for research into metabolic disorders and thyroid function modulation. -
β-Catenin Modulator
β-Catenin modulator-5, a selective modulator of β-Catenin, exhibits potent activity in regulating this key signaling pathway involved in cell proliferation and differentiation. This compound, characterized by its oxazole and thiazole structure, is valuable for research applications focused on cancer biology, developmental processes, and tissue homeostasis. Its ability to effectively manipulate β-Catenin activity makes it a crucial tool for investigating Wnt signaling-related mechanisms in various biological systems. -
β-Catenin Modulator
β-Catenin modulator-3 is a selective modulator of β-Catenin, characterized by its unique oxazole and thiazole chemical structure. This compound demonstrates significant biological activity in regulating β-Catenin signaling pathways, making it a valuable tool for research in cancer biology and developmental studies. Its ability to modulate the Wnt/β-Catenin pathway positions it as a potential candidate for studies targeting various cancers and neurodegenerative diseases. -
Axin Phosphorylation Inhibitor; β-catenin Phosphorylation Inhibitor
FRATtide is a peptide inhibitor targeting GSK-3, effectively disrupting the phosphorylation of Axin and β-catenin. By preventing the binding of GSK-3 to Axin, FRATtide modulates the Wnt signaling pathway, making it a valuable tool for research in cancer biology and developmental processes. This reagent is essential for studying mechanisms of β-catenin regulation and its implications in various diseases. -
β-Catenin Modulator
β-Catenin modulator-7 is a targeted modulator of β-catenin, primarily influencing its expression in the cytoplasm and nucleus of HCT-116 cells. This compound effectively inhibits GSK 3β phosphorylation, promoting nitric oxide release and thereby reducing cancer cell proliferation with an IC50 of 0.6-0.9 μM. β-Catenin modulator-7 is positioned for research applications in studying colon cancer and its associated signaling pathways. -
Wnt Inhibitor
Jatrophone is a diterpenoid that functions as a Wnt inhibitor, exhibiting significant anticancer activity. Isolated from Jatropha isabelli, Jatrophone disrupts the Wnt/β-catenin signaling pathway, leading to a reduction in cell proliferation and inhibition of epithelial-mesenchymal transition (EMT) in triple-negative breast cancer cells. This compound is valuable for research focused on cancer biology and therapeutic strategies targeting Wnt pathway modulation. -
β-catenin Inhibitor
NLS-StAx-h is a selective β-catenin inhibitor designed to disrupt Wnt signaling pathways. This cell-permeable, stapled peptide exhibits an IC50 of 1.4 μM, effectively blocking β-catenin-transcription factor interactions. NLS-StAx-h demonstrates potent anti-proliferative effects on cancer cells, making it a valuable tool for research in cancer biology and therapeutic applications targeting aberrant Wnt signaling. -
GSK-3β Inhibitor
GSK-3β inhibitor 24 is a highly potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 0.22 nM. This compound effectively enhances GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner, while reducing hyperphosphorylation of tau protein, specifically lowering p-tau-Ser396 levels. Additionally, GSK-3β inhibitor 24 promotes the upregulation of β-catenin and neurogenesis-related markers such as GAP43 and MAP-2, making it a valuable tool in Alzheimer's disease research and therapeutic studies. -
β-Catenin Modulator
β-Catenin modulator-4 is a selective modulator of the β-Catenin signaling pathway. It exhibits strong potency in regulating β-Catenin activity, making it valuable for studies of cellular processes such as proliferation and differentiation. This compound is particularly relevant for research on developmental biology, cancer, and tissue regeneration, where β-Catenin plays a critical role in signaling dynamics. -
Wnt/β-Catenin Inhibitor
YW2036 is a potent inhibitor of the Wnt/β-Catenin signaling pathway, exhibiting an IC50 value of 637 nM. This compound has significant biological activity and is primarily utilized in research focused on colorectal cancer (CRC). Its role as a Wnt/β-Catenin inhibitor makes it a valuable tool for studies investigating the mechanisms underlying CRC progression and treatment approaches. -
β-catenin/Tcf4 Inhibitor
BC21 (NSC 109268) is a β-catenin/Tcf4 inhibitor with an IC50 of 5 μM. It disrupts the interaction between β-catenin and Tcf4-derived peptides, thereby inhibiting β-catenin/Tcf4-mediated transcriptional activity. This compound is particularly valuable in cancer research, where aberrant β-catenin signaling plays a critical role in tumor progression. -
Wnt/β-catenin Inhibitor
hsBCL9CT-24 is a potent inhibitor of the Wnt/β-catenin signaling pathway, targeting β-catenin to modulate oncogenic processes. This compound has demonstrated significant anti-tumor activity by reactivating the anti-cancer immune response impaired by aberrant Wnt signaling. hsBCL9CT-24 is applicable in cancer research, particularly in studies exploring Wnt pathway inhibition and immune evasion in tumor microenvironments. -
β-Catenin Modulator
β-Catenin modulator-2 is a selective modulator of β-Catenin, primarily targeting the Wnt signaling pathway. This compound, characterized by its oxazole and thiazole structure, exhibits significant biological activity in regulating β-Catenin levels. It is suitable for research applications aimed at studying cellular processes involved in cancer, developmental biology, and tissue regeneration. -
β-Catenin Modulator
β-Catenin modulator-1 (IIa-650) is a potent modulator of β-Catenin, a crucial component in the Wnt signaling pathway. It demonstrates significant biological activity in the regulation of cell proliferation and differentiation, making it invaluable for cancer research. This compound is utilized to investigate β-Catenin's role in tumorigenesis and other related pathologies, providing insights into therapeutic strategies targeting this pathway. -
Wnt/β-catenin Inhibitor
1(R),2(S)-epoxy Cannabidiol is a potent inhibitor of the Wnt/β-catenin signaling pathway. This structural analogue of phytocannabinoids demonstrates significant biological activity, making it a valuable tool for research in neuroprotection. Its ability to modulate this critical pathway positions it as a promising candidate for studies focused on neuroprotective agents. -
β-catenin/Tcf4 Inhibitor
Murayaquinone is a potent inhibitor of the β-catenin/Tcf4 complex, exhibiting an IC50 of 2.4 μM. This compound, derived from Streptomyces sp. AN140557, demonstrates significant nematicidal activity. It serves as a valuable tool for research applications focused on Wnt signaling pathways and their roles in developmental biology and cancer research. -
β-Catenin Modulator
β-Catenin modulator-8 is a small molecule that functions as a β-Catenin modulator, primarily targeting the Wnt signaling pathway. It exhibits significant potential in altering β-Catenin activity, making it a valuable tool for research in cancer biology. This compound can be utilized in studies aimed at understanding tumorigenesis, as well as in the development of therapeutic strategies targeting β-Catenin-related malignancies. -
Wnt/β-catenin Inhibitor
Sempervirine nitrate is a Wnt/β-catenin pathway inhibitor derived from the alkaloid Gelsemium elegans Benth. This compound exhibits significant anti-proliferative effects on hepatocellular carcinoma (HCC) cells and promotes apoptosis through modulation of the Wnt/β-catenin signaling cascade. Sempervirine nitrate is valuable for research into cancer biology and therapeutic approaches targeting HCC. -
β-catenin Modulator
β-Catenin modulator IIa-661 is a selective modulator of β-catenin, targeting its activity and inhibiting the Wnt/wingless (wg) signaling pathway. This compound is instrumental in cancer research, providing insights into β-catenin's role in tumor progression and cellular signaling. Its application may aid in developing therapeutic strategies for cancers characterized by aberrant Wnt signaling. -
Wnt/β-catenin Activator
Astragaloside I is a Wnt/β-catenin activator known for its osteogenic properties. It promotes osteoblast differentiation by enhancing the Wnt/β-catenin signaling pathway. This compound is valuable for research focused on bone development, regeneration, and related signaling mechanisms in various biological systems. -
Notch Inhibitor
Prednisone acetate is a glucocorticoid that functions as an orally active Notch inhibitor. It exhibits significant anti-inflammatory activity and has the potential to enhance immune responses. This compound is widely used in research to investigate its effects on Notch signaling and its implications in various inflammatory and immune-related conditions. -
γ-Secretase Inhibitor I
Z-LLNle-CHO is a γ-secretase inhibitor that effectively disrupts the Akt-mediated pro-survival signaling pathway, leading to caspase activation and ROS-dependent apoptosis. This compound is instrumental in cancer research, particularly in the studies of breast cancer and leukemia, where inhibiting γ-secretase activity may provide insights into therapeutic strategies. -
CK2 Inhibitor
CX-5011 is a selective inhibitor of casein kinase 2 (CK2), a serine/threonine kinase involved in cellular signaling pathways. This compound has been shown to activate Rac1, leading to effects on cell motility and morphology. Notably, CX-5011 induces apoptosis in various cancer cell lines, thereby promoting cancer cell death and making it a valuable tool for research in cancer biology and therapeutic interventions targeting CK2. -
GSK-3α/β Selective Inhibitor
GSK-3α/β-IN-1 is a selective inhibitor of glycogen synthase kinase-3 alpha and beta (GSK-3α/β), demonstrating IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. Additionally, GSK-3α/β-IN-1 exhibits PKA inhibition with an IC50 of 0.188 μM. This compound effectively reduces cell viability in several glioblastoma (GBM) cell lines, with IC50 values ranging from 3 to 6 μM over 72 hours, while displaying minimal toxicity to human astrocytes. GSK-3α/β-IN-1 also shows promising central nervous system activity in human blood-brain barrier models of GBM, supporting its potential as a therapeutic agent in cancer research. -
PKG/PKA Activator
Sp-8-pCPT-cGMPS is a potent activator of protein kinase G (PKG) and protein kinase A (PKA) with significant cell membrane permeability and phosphodiesterase stability. This cyclic guanosine monophosphate analog effectively engages PKG types I α, I β, and II, making it invaluable for research in signal transduction pathways. It is utilized to investigate the role of cGMP in neural plasticity, synaptic transmission, and other physiological processes influenced by these kinases. -
γ-Secretase Inhibitor
EVP-0015962 is a potent γ-secretase inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 value of 3.9 μM. By modulating the γ-secretase-mediated cleavage of amyloid precursor protein, EVP-0015962 decreases the production of Aβ42 while increasing Aβ38 levels. This compound has demonstrated efficacy in reducing amyloid aggregates, mitigating amyloid plaque formation, and lowering inflammatory markers in mouse models, thereby enhancing cognitive function. EVP-0015962 serves as a valuable tool in Alzheimer's disease research. -
γ-Secretase Modulator
AZ1136 is a selective γ-secretase modulator (GSM) that effectively reduces the levels of amyloid-beta peptides Aβ42 and Aβ40, with IC50 values of 990 nM and 1400 nM, respectively. Furthermore, AZ1136 increases levels of Aβ39 and Aβ37 while showing no effect on Aβ38. This compound is valuable for research applications investigating the pathogenesis of Alzheimer's disease and the modulation of amyloid-beta metabolism. -
γ- Secretase Modulator
BIIB042 is a selective γ-secretase modulator that effectively alters the processing of amyloid precursor protein, resulting in decreased levels of Aβ42 and increased levels of Aβ38. This compound demonstrates significant brain penetration and has shown efficacy in reducing brain Aβ42 levels in CF-1 mice and Fischer rats, while also lowering plasma Aβ42 levels in cynomolgus monkeys. Additionally, BIIB042 decreases Aβ42 levels and ameliorates Aβ plaque burden in Tg2576 mouse models. This reagent is valuable for research into Alzheimer’s disease. -
γ-secretase Modulator
(E/Z)-Sulindac sulfide is a selective γ-secretase modulator that plays a crucial role in the modulation of amyloid-beta (Aβ) peptide production. This compound notably reduces the production of Aβ42, favoring the generation of shorter Aβ species, making it a valuable tool for research into Alzheimer's disease. Its ability to influence Aβ processing makes (E/Z)-Sulindac sulfide significant for studies focusing on Alzheimer's pathogenesis and potential therapeutic strategies. -
γ-secretase Inhibitor
JNJ-40418677 is a potent orally active inhibitor of γ-secretase, capable of crossing the blood-brain barrier. It effectively inhibits the production of Aβ42 and the activity of NS2B-NS3 protease, with IC50 values of 200 nM and 3.9 μM, respectively. This compound exhibits favorable biological tolerance and is suitable for research applications related to Alzheimer's disease. -
γ-Secretase Modulator
PF-06648671 is an orally active γ-secretase modulator that effectively penetrates the blood-brain barrier. This compound demonstrates the ability to reduce levels of amyloid-beta peptides Aβ42 and Aβ40, while concurrently increasing Aβ37 and Aβ38 in vitro. PF-06648671 is valuable for research applications focused on Alzheimer’s disease and the modulation of amyloid processing pathways. -
γ-secretase Inhibitor
Sulindac sulfide is a noncompetitive inhibitor of γ-secretase, exhibiting an IC50 of 20.2 μM for γ42-secretase activity. This compound plays a crucial role in research involving Alzheimer's disease and other neurodegenerative conditions by modulating the processing of amyloid precursor protein. Its ability to inhibit γ-secretase makes it a valuable tool for studies focused on reducing amyloid-beta peptide formation and investigating related signaling pathways. -
γ-secretase Inhibitor
ELND 006 is a selective γ-secretase inhibitor that effectively reduces amyloid beta (Aβ) generation while preserving Notch signaling pathways. Developed with a focus on metabolic stability, this compound has shown significant efficacy in lowering Aβ levels both in vitro and in vivo during preclinical studies. ELND 006, alongside its structural analog ELND 007, has advanced into human clinical trials, indicating its potential therapeutic applications in Alzheimer's disease research and treatment. -
γ-secretase Modulator
RO7185876 is a selective gamma-secretase modulator that plays a crucial role in the regulation of amyloid precursor protein processing. This compound is primarily investigated for its potential in Alzheimer's disease research, where it may help reduce the production of amyloid-beta peptides. Its unique mechanism of action positions RO7185876 as a valuable tool for studying the pathophysiology of Alzheimer's and exploring therapeutic options. -
γ-secretase Modulator
GSM-1 is a potent γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1). By modulating γ-secretase activity, GSM-1 influences the processing of amyloid precursor protein (APP), making it valuable in Alzheimer's disease research. This compound can be utilized to investigate mechanisms of amyloid-beta peptide generation and potential therapeutic strategies for neurodegenerative disorders. -
gamma-Secretase Inhibitor
Gamma-secretase modulator 6 is a gamma-secretase inhibitor that effectively reduces the secretion of Aβ42 in HEK cells stably expressing amyloid precursor protein (APP), with a pIC50 value of 8.1. This compound plays a crucial role in the study of Alzheimer's disease by modulating gamma-secretase activity, thereby influencing amyloid plaque formation. It is a valuable tool for researchers exploring therapeutic strategies targeting amyloid pathology in neurodegenerative disorders. -
γ-secretase Modulator
FRM-024 is a potent γ-secretase modulator designed for central nervous system applications. It selectively alters the activity of γ-secretase, a critical enzyme involved in the pathogenesis of familial Alzheimer’s disease. This compound has demonstrated the ability to influence amyloid precursor protein processing, making it a valuable tool for research focused on Alzheimer’s therapeutics and disease mechanisms. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-2 is a selective γ-secretase inhibitor that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 226 nM. This compound demonstrates potential for research applications in Alzheimer's disease and other conditions associated with Aβ deposition. Its ability to modulate γ-secretase activity makes it a valuable tool for studying the mechanisms underlying amyloid-related pathologies. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-3 is a selective inhibitor of γ-secretase that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 148 nM. By modulating γ-secretase catalytic activity, it decreases Aβ42 production and helps mitigate the neurotoxicity associated with amyloid deposition. This compound shows potential for research applications in Alzheimer's disease (AD) studies. -
γ-secretase Inhibitor
ELN318463 is a selective inhibitor of γ-secretase, targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin 1 (PS1) and presenilin 2 (PS2) γ-secretase complexes, with EC50 values of 12 nM and 656 nM, respectively, showcasing a 51-fold greater selectivity for PS1. This compound is primarily utilized in research focused on Alzheimer's disease and related neurodegenerative disorders, making it a valuable tool for studies investigating APP processing and amyloid plaque formation. -
γ-secretase Modulator
(-)-FRM-024 is a potent γ-secretase modulator that effectively penetrates the central nervous system. This compound is instrumental in Alzheimer’s disease research, facilitating the study of amyloid precursor protein processing and its implications in neurodegeneration. Its ability to modulate γ-secretase activity makes it a valuable tool for exploring therapeutic interventions in Alzheimer's pathology. -
γ-Secretase Modulator
γ-Secretase modulator 4 is a potent modulator of the γ-secretase enzyme, characterized by its ability to effectively reduce Aβ42 peptide levels with IC50 values of 0.014 μM in human samples and 0.017 μM in mouse samples. This compound has significant implications in Alzheimer's research, particularly in the study of amyloid-beta production and the related pathophysiology. Its mechanism of action makes it a valuable tool for investigations into therapeutic strategies targeting Alzheimer's disease. -
γ-secretase Inhibitor
(9R)-RO7185876 is a selective inhibitor of γ-secretase, targeting the cleavage of amyloid precursor protein. This compound significantly reduces the secretion of Aβ42 peptides, making it a valuable tool for research on Alzheimer's disease and related disorders, such as cerebral amyloid angiopathy and multi-infarct dementia. Additionally, (9R)-RO7185876 may be utilized to investigate conditions associated with amyloid deposition, including dementia pugilistica and Down syndrome. -
Gamma-Secretase Modulator
Gamma-Secretase Modulator 1 Hydrochloride acts as a modulator of gamma-secretase, a crucial enzyme implicated in the pathogenesis of Alzheimer's disease. This compound is designed to influence the processing of amyloid precursor protein (APP), ultimately affecting the production of amyloid-beta peptide. Its potential applications include studying the modulation of amyloid-beta levels and investigating therapeutic strategies for Alzheimer's disease and related neurodegenerative disorders. -
γ-secretase Modulator
Nivegacetor is a potent γ-secretase modulator that plays a critical role in the modulation of amyloid precursor protein processing. By influencing the activity of γ-secretase, Nivegacetor is valuable for research into Alzheimer's disease and other neurodegenerative conditions. Its ability to alter the production of amyloid-beta peptides makes it a useful tool for exploring therapeutic pathways and understanding the molecular mechanisms underlying these diseases. -
γ-Secretase Modulator
Aβ42-IN-1 is a potent γ-secretase modulator (GSM) designed to target the enzymatic cleavage of amyloid precursor protein, effectively lowering amyloid-beta 42 (Aβ42) levels. With an IC50 value of 0.091 μM, Aβ42-IN-1 demonstrates significant inhibition of Aβ42 production while avoiding CYP3A4 inhibition, indicating a favorable safety profile. Its sustained pharmacokinetic properties make it a valuable tool for research into Alzheimer's disease and related neuropathologies. This compound holds promise for exploring therapeutic strategies aimed at modulating γ-secretase activity in neurodegenerative disorders.
