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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
YAP Inhibitor
Hirudin (54-65) is a potent thrombin antagonist and YAP inhibitor that exhibits anticoagulatory properties. By blocking the anion binding site of thrombin, it inhibits both soluble and thrombus-bound thrombin, subsequently reducing YAP expression, nuclear translocation, and downstream signaling in vascular endothelial cells. This compound is employed in research related to liver obstructive cholestasis and liver fibrosis, as it ameliorates fibrosis symptoms, attenuates angiogenesis, and decreases inflammation and tissue hypoxia. Furthermore, Hirudin (54-65) promotes extracellular calcium influx in vascular smooth muscle, facilitating endothelium-independent contraction. -
Notch1 Inhibitor
NADI-351 is a potent orally active inhibitor of Notch1, specifically designed to disrupt Notch1 transcription complexes and decrease its recruitment to target genes. This compound exhibits significant efficacy in inhibiting Notch1 signaling pathways, making it a valuable tool for cancer research. Its selective action provides insights into the role of Notch1 in tumorigenesis and related cellular processes. -
Notch1 Inhibitor
ASR-490 is a selective Notch1 inhibitor that effectively reduces the viability of HCT116 and SW620 cancer cell lines by downregulating Notch1 signaling pathways. This compound successfully impedes tumor growth in both control cells and Notch1-overexpressing HCT116 transfectants. In vivo studies demonstrate that ASR-490 significantly inhibits tumor growth in xenograft models, highlighting its potential as a therapeutic agent in cancer research. -
Notch1 Inhibitor
Procyanidin B2 3,3'-di-O-gallate is a selective Notch1 inhibitor that demonstrates significant biological activity against cancer stem cells, particularly in prostate cancer. This compound effectively targets both unsorted and sorted cancer stem cells at lower concentrations. By suppressing the activated Notch1 signaling pathway, including responses induced by the Jagged1 ligand, Procyanidin B2 3,3'-di-O-gallate is a valuable tool for research focused on cancer biology and therapeutic development. -
Gli1-DNA Interaction Inhibitor
Glabrescione B is a Gli1-DNA interaction inhibitor that targets the Hedgehog (Hh) signaling pathway. This compound disrupts the activity of Gli1 by preventing its binding to DNA, thereby inhibiting the growth of Hedgehog-dependent tumor cells. Additionally, Glabrescione B impairs the self-renewal capacity and clonogenic potential of tumor-derived stem cells, making it a valuable tool for studying Hh-related cancers and stem cell biology. -
3MST Inhibitor
I3MT-3 is a selective inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST), exhibiting an IC50 value of 2.7 μM, demonstrating its potency against this target. The compound selectively interacts with a persulfurated cysteine residue within the active site of 3MST, ensuring minimal off-target activity. I3MT-3 is ideal for studies investigating the role of hydrogen sulfide and its metabolic pathways, as well as potential therapeutic applications related to sulfur metabolism. -
MST1 Inhibitor
IHMT-MST1-58 is a potent and selective inhibitor of the mammalian STE20-like protein 1 kinase (MST1), demonstrating an IC50 value of 23 nM. This compound is valuable for investigating the role of MST1 in cellular signaling pathways and can be utilized in research focused on Type 1 and Type 2 diabetes. Its oral bioavailability makes it suitable for in vivo studies aimed at elucidating the therapeutic potential of targeting MST1 in metabolic disorders. -
3-MST Inhibitor
BRD2577 is a selective inhibitor of mercaptopyruvate sulfurtransferase (3-MST) with an IC50 value of 9.9 μM. This compound effectively reduces hydrogen sulfide (H2S) production in colon carcinoma cells, providing insights into the metabolic pathways associated with this cancer type. While BRD2577 shows minimal impact on colon cancer cell proliferation and mitochondrial function, it serves as a valuable tool for investigating the role of H2S in colon cancer biology and therapeutic strategies. -
MST3 Inhibitor
JA310 is a selective MST3 kinase inhibitor, demonstrating high cellular potency with an EC50 value of 106 nM. This compound serves as a valuable tool in studying MST3's role in cellular signaling pathways and its involvement in various diseases. JA310 can be utilized in research applications focused on the modulation of MST3 activity and its effects on cell proliferation, survival, and migration. -
MST3/4 Inhibitor
MR24 is a selective inhibitor of mammalian STE20-like kinases MST3 and MST4. It demonstrates an EC50 of 57 nM for MST3 and 583 nM for MST4, highlighting its targeted activity. MR24 induces G1 phase cell cycle arrest, making it a valuable tool for investigating cell cycle regulation. This compound is particularly relevant for cancer research, including studies focused on breast, liver, and lung cancers. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-β signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
PKG Inhibitor
Rp-8-pCPT-cGMPS sodium is a selective inhibitor of cGMP-dependent protein kinase (cGK), functioning primarily through the modulation of cGMP signaling pathways. This compound also acts as an agonist for cyclic nucleotide-gated (CNG) channels in a voltage-dependent manner, making it valuable for studying the intricate roles of cyclic nucleotides in cellular processes. Its applications extend to research in cardiovascular physiology, neurobiology, and signal transduction mechanisms. -
PKG1α Inhibitor
DT-3 is a selective inhibitor of protein kinase G Iα (PKG Iα), designed to impede the cGMP-PKG signaling pathway. This membrane-permeable peptide demonstrates significant pharmacological activity, making it valuable for research applications focused on cardiovascular function and signaling related diseases. DT-3 enables the investigation of the roles of PKG Iα in various cellular processes and helps elucidate its contributions to cardiovascular health and disease. -
PKG Inhibitor
Rp-8-pCPT-cGMPS is a competitive inhibitor of cGMP-dependent protein kinase (PKG) with a Ki value of 0.5 μM. Its high lipid solubility facilitates cellular penetration, enabling effective inhibition of PKG activity within cells. This reagent is valuable for investigating the role and function of PKG in cellular processes, particularly in platelets. -
SGK1/GSK3β Inhibitor
SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders.
