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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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 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 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. -
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/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 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. -
γ-secretase Inhibitor
MK-0752 sodium is a potent, orally bioavailable inhibitor of γ-secretase, exhibiting a dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. This compound effectively crosses the blood-brain barrier and demonstrates the ability to decrease newly generated central nervous system Aβ levels in vivo. MK-0752 sodium is primarily utilized in research on Alzheimer’s disease and other neurodegenerative disorders linked to amyloid-beta pathology. -
γ-secretase Inhibitor
γ-Secretase modulator 11 functions as a potent γ-secretase inhibitor, effectively reducing levels of amyloid beta 42 in vitro and demonstrating significant brain penetration. This compound exhibits minimal inhibition of cytochrome P450 enzymes, highlighting its selective profile. Additionally, γ-secretase modulator 11 has shown considerable efficacy in alleviating cognitive deficits in Alzheimer's disease model mice, making it a valuable tool for research in neurodegenerative disorders. -
γ-Secretase Inhibitor
GSI-18 is a potent γ-secretase inhibitor that disrupts Notch signaling, contributing to its anticancer properties. This compound effectively inhibits the attachment-free growth of pancreatic cancer cells, making it valuable for research into cancer biology and therapeutic interventions. Its mechanism of action offers insights into the regulation of cell proliferation and differentiation in oncogenic contexts. -
γ-secretase Inhibitor
ELND 007 is a selective γ-secretase inhibitor that primarily targets the reduction of amyloid beta (Aβ) generation while minimizing inhibition of Notch signaling. It demonstrates significant biological activity in both in vitro and in vivo settings, effectively decreasing Aβ levels. This compound has shown potential therapeutic benefits for Alzheimer’s disease, particularly as evidenced by reductions in Aβ levels observed in cerebrospinal fluid during human clinical trials, following a strategic emphasis on metabolic stability and chirality in its development. -
γ-secretase Inhibitor
γ-Secretase-IN-2 is a potent inhibitor of γ-secretase, demonstrating an IC50 of 0.06 nM. This compound is instrumental in researching Alzheimer's disease, providing insights into the enzymatic processes involved in neurodegeneration. Its high efficacy makes it a valuable tool for studying the pathophysiology of Alzheimer's and exploring potential therapeutic strategies. -
γ-secretase Inhibitor
LY3056480 is a potent γ-secretase inhibitor that targets Notch signaling pathways. This compound has demonstrated efficacy in enhancing recovery from mild to moderate sensorineural hearing loss, while exhibiting a favorable safety profile. Additionally, intratympanic administration of LY3056480 has been shown to promote hair cell regeneration and contribute to partial auditory recovery in mammalian models, making it a valuable tool for research in hearing restoration and neurodegenerative studies. -
γ-secretase Inhibitor
III-31-C is a hydroxyethyl urea-based inhibitor of γ-secretase. It demonstrates potent inhibition of amyloid-beta (Aβ) production, with an IC50 value of 10 nM in a cell-free γ-secretase assay and 200 nM in APP-transfected cells. This compound is relevant for research focused on Alzheimer's disease and offers valuable insights into the modulation of Aβ metabolism. -
γ-secretase Inhibitor
LY-411575 (isomer 2) is a potent inhibitor of γ-secretase, an enzyme involved in the cleavage of amyloid precursor protein and a key player in the pathogenesis of Alzheimer's disease. This compound has been shown to effectively reduce the production of amyloid-beta peptides, making it valuable for research into therapeutic strategies for neurodegenerative disorders. Its selective inhibition of γ-secretase also facilitates the study of its role in cellular signaling and development. -
γ-secretase Inhibitor
GSI-136 is a potent inhibitor of γ-secretase, exhibiting an IC50 of 3 nM. This compound effectively reduces Aβ40 levels in diethylamine-extracted brain homogenates from C57BL/6 mice in a dose-dependent manner. GSI-136 serves as a valuable tool in medicinal chemistry and Alzheimer’s disease research, aiding in the exploration of therapeutic strategies targeting amyloid-beta production. -
γ-secretase Inhibitor
LY-411575 (isomer 3) is a potent inhibitor of γ-secretase, an enzyme complex involved in the proteolytic processing of various transmembrane proteins, including amyloid precursor protein (APP). This compound is utilized in research studying Alzheimer's disease and other conditions associated with aberrant Notch signaling. Its ability to modulate γ-secretase activity makes it a valuable tool for investigating the therapeutic potential of targeting this pathway. -
γ-secretase Inhibitor
ELN318463 racemate is a selective γ-secretase inhibitor targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin (PS1) and PS2-comprised γ-secretase, with EC50 values of 12 nM for PS1 and 656 nM for PS2, indicating a 51-fold selectivity for PS1. This compound is useful in research applications focused on Alzheimer's disease and the modulation of amyloid beta peptide production. -
CK1δ/1ε Inhibitor
SR-2890 is a highly selective ATP-competitive inhibitor of casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ε), exhibiting IC50 values of 4 nM and 44 nM, respectively. This compound effectively inhibits the serine/threonine kinase activity of CK1δ and has demonstrated antiproliferative effects against human A375 melanoma cells. Additionally, SR-2890 has shown potential utility in research related to melanoma and in studying diseases associated with CK1δ/ε, such as Alzheimer's disease, due to its favorable in vivo pharmacokinetic properties and metabolic stability. -
Hedgehog Inhibitor
TPB15 is a potent inhibitor of Hedgehog (Hh) signaling, specifically targeting Smoothened (Smo). This compound effectively induces cell cycle arrest and apoptosis in MDA-MB-468 breast cancer cells by blocking Smo translocation into cilia and reducing the expression of Smo protein and mRNA. Additionally, TPB15 downregulates glioma-associated oncogene 1 (Gli1), a key downstream regulator. TPB15 demonstrates significant anti-tumor activity with a favorable toxicity profile, making it a valuable tool for cancer research focused on Hedgehog pathway modulation. -
p38/CK1 Inhibitor
Casein kinase 1δ-IN-29 is a potent inhibitor of p38α and casein kinase 1, demonstrating IC50 values of 0.041 µM for p38α, 0.005 µM for CK1δ, and 0.447 µM for CK1ε. This compound effectively interrupts the cell cycle at the subG1 phase and induces apoptosis in AC1-M88 cells. It serves as a valuable tool in research applications focused on cell cycle regulation and apoptosis pathways. -
β-catenin Inhibitor
β-catenin-IN-9 is a potent inhibitor of β-catenin, a key regulator in various signaling pathways. It has been shown to induce apoptosis and cell cycle arrest, while effectively inhibiting migration, invasion, and epithelial-mesenchymal transition (EMT) in colorectal cancer cells. Additionally, β-catenin-IN-9 suppresses the transcription of β-catenin and vimentin, leading to significant reductions in β-catenin protein levels. This reagent is valuable for research focused on colorectal cancer and related signaling pathways. -
Hsp90-Cdc37 PPI Inhibitor
Hsp90-Cdc37-IN-4 is a selective inhibitor of the Hsp90-Cdc37 protein-protein interaction (PPI). This compound disrupts the interaction by inhibiting casein kinase 2 (CK2), leading to reduced phosphorylation of Cdc37 at Serine 13. In cellular assays, Hsp90-Cdc37-IN-4 has been shown to induce G0/G1 cell cycle arrest and activate apoptotic pathways via the mitochondria. Additionally, it exhibits significant anti-breast cancer properties, making it a valuable tool in cancer research. -
γ-secretase Inhibitor
MRK 003 is a selective and orally bioavailable inhibitor of γ-secretase. It demonstrates significant reduction of Aβ peptide production in the brain in vivo, making it a valuable tool for Alzheimer's disease research. Additionally, MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation both in vitro and in vivo, supporting its potential applications in cancer research. -
CK1ε Inhibitor
Orobol is a selective inhibitor of Casein Kinase 1 epsilon (CK1ε) with demonstrated anti-skin-aging and anti-obesity effects. It targets multiple kinases, including VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK, exhibiting inhibitory activity with IC50 values ranging from 1.24 to 4.45 μM. Additionally, Orobol inhibits various phosphoinositide 3-kinase (PI3K) isoforms, specifically showing activity with IC50 values between 3.46 and 5.27 μM for PI3K α/β/γ/K/δ. These properties make Orobol valuable for investigating signaling pathways related to cellular growth, metabolism, and aging. -
Fyn/GSK-3β Inhibitor
Fyn-IN-1 is a selective inhibitor of Fyn and GSK-3β, demonstrating IC50 values of 0.044 μM and 0.61 μM, respectively. This compound effectively downregulates the expression of the pro-inflammatory enzyme iNOS, making it a valuable tool in studying neuroinflammatory processes. Fyn-IN-1 is particularly relevant for research focused on neurodegenerative diseases, providing insights into potential therapeutic interventions. -
DYRK1A/GSK3β Inhibitor
GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways. -
GSK-3β/FYN Inhibitor
ARN25068 is a sub-micromolar inhibitor targeting the protein kinases GSK-3β, FYN, and DYRK1A. It plays a significant role in modulating tau hyperphosphorylation, which is implicated in neurodegenerative diseases. This compound is valuable for research applications focused on neurobiology and pathology related to tau protein and related neurodegenerative processes. -
Casein Kinase/DYRK/TNIK Inhibitor
ON 108600 is a potent inhibitor of casein kinase 2 (CK2), TYRK1 (DYRK), and TNIK, demonstrating IC50 values of 0.016 μM against DYRK1A, 0.007 μM against DYRK2, 0.05 μM against CK2α1, 0.005 μM against CK2α2, and 0.005 μM against TNIK. This compound exhibits promising antitumor activity, making it a valuable tool for research applications focused on cancer biology, signaling pathways, and kinase inhibition studies. Its specificity for these kinases positions ON 108600 as a critical reagent for investigating therapeutic strategies targeting kinase-related diseases. -
GSK3 Inhibitor
GSK3-IN-10 is a potent inhibitor of glycogen synthase kinase 3 (GSK3) isoforms α and β, demonstrating IC50 values of 1.0 nM and 2.0 nM, respectively. This compound effectively inhibits the activation of β-catenin, thereby promoting neuronal survival and providing a protective effect against endoplasmic reticulum stress. GSK3-IN-10 is valuable for research applications focused on neuroprotection and cellular stress response mechanisms. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
Hedgehog signaling inhibitor
Cyclopamine is a Smo or hedgehog signaling pathway inhibitor.
