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Catalog No.
Product Name
Application
Product Information
Citations
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GSK-3β Inhibitor
ZDWX-25 is a potent dual inhibitor of GSK-3β and DYRK1A, demonstrating an IC50 value of 71 nM for GSK-3β. This compound exhibits significant cytotoxic effects on SH-SY5Y and HL-7702 cell lines, making it a valuable tool for research in neurodegenerative diseases such as Alzheimer's disease. Its inhibitory action on key kinase pathways suggests potential for further exploration in therapeutic applications. -
GSK-3β/CDK-2/CDK-4 Inhibitor
UNC10112785 is a potent inhibitor of serine/threonine kinases, specifically targeting GSK-3β, CDK-2, and CDK-4 with IC50 values of 0.031 μM, 0.016 μM, and 1.99 μM, respectively. This compound exhibits significant biological activity that positions it as a valuable tool in the study of type 2 diabetes. Its ability to modulate key pathways involved in metabolic regulation makes it an essential reagent for researchers investigating therapeutic interventions in diabetic conditions. -
GSK-3 Inhibitor
BRD1652 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3), a critical regulator in various signaling pathways. This compound has shown potential in modulating GSK-3 activity, making it a valuable tool for investigating the molecular mechanisms underlying emotion-related disorders. Its application can enhance research on neuropsychiatric conditions and therapeutic strategies targeting GSK-3 signaling. -
GSK-3β Inhibitor
Dihydronarwedine is an inhibitor of glycogen synthase kinase-3β (GSK-3β). At a concentration of 10 μM, it demonstrates a 39% reduction in GSK-3β activity. This compound is useful in research applications related to cellular signaling pathways, neurodegenerative diseases, and cancer therapy, where GSK-3β modulation is of interest. -
GSK-3 Inhibitor
GSK-3 inhibitor 7 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3), a key regulator in various cellular processes. This compound demonstrates significant activity in modulating GSK-3 signaling pathways, making it a valuable tool for research in neurobiology and related fields. Its application may enhance understanding of GSK-3's role in neurodegenerative diseases and neuronal signaling. -
GSK-3 Inhibitor
Cazpaullone is a potent glycogen synthase kinase-3 (GSK-3) inhibitor that plays a critical role in cellular signaling pathways. It enhances pancreatic beta cell protection and promotes their replication, making it valuable in diabetes research. Cazpaullone's mechanism of action provides insights into potential therapeutic strategies for diabetes and related metabolic disorders. -
GSK-3β Inhibitor
GSK-3β inhibitor 25 primarily targets glycogen synthase kinase 3 beta (GSK-3β), demonstrating weak inhibitory activity with an IC50 greater than 100 μM. This compound is utilized in biochemical research to elucidate the role of GSK-3β in various signaling pathways and cellular processes, including metabolism and cell proliferation. Its modest potency may serve as a lead in the development of more selective GSK-3β inhibitors for therapeutic applications. -
GSK-3β Inhibitor
GSK-3β inhibitor 26 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 18.23 μM. This compound is instrumental in research focusing on cancer, inflammation, and neurodegenerative diseases, facilitating the exploration of therapeutic pathways and mechanisms associated with GSK-3β modulation. -
GSK-3β Inhibitor
TD114-2 is a potent and highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β), exhibiting an IC50 value of 48 nM. The compound forms a key hydrogen bond with arginine 141, which contributes to its remarkable specificity for GSK-3β compared to other kinases. TD114-2 is a valuable tool for investigating the role of GSK-3β in various conditions, including diabetes, neurodegenerative diseases, and other disorders linked to GSK-3β dysregulation. -
PI4Kβ/PKG Inhibitor
PI4Kβ/PKG-IN-2 is a potent dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). This compound demonstrates significant inhibitory activity against Plasmodium, making it a valuable tool for investigating malaria pathogenesis and potential therapeutic strategies. Its oral bioavailability further supports its use in preclinical studies aimed at understanding malaria biology. -
PfGSK3/PfPK6 Inhibitor
PfGSK3/PfPK6-IN-1 is a selective inhibitor targeting PfGSK3 and PfPK6, with IC50 values of 97 nM and 8 nM, respectively. This compound effectively inhibits the proliferation of blood-stage Plasmodium falciparum 3D7 parasites, making it a valuable tool for malaria research. Additionally, PfGSK3/PfPK6-IN-1 exhibits low cytotoxicity in hepatocyte cultures at concentrations up to 200 nM, with a significant reduction in cell viability observed at 2 μM. Its dual action enhances its potential in studying malaria-related mechanisms and potential therapeutic strategies. -
PKG Inhibitor
Protein kinase G inhibitor-2 is a selective inhibitor of mycobacterial protein kinase G, exhibiting an IC50 value of 3 μM. This compound is utilized in the investigation of mycobacterial infections and their associated signaling pathways. Its efficacy as a PKG inhibitor supports research into therapeutic strategies targeting mycobacterial diseases. -
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. -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
p38 MAPK inhibitor
SB 203580 hydrochloride (Adezmapimod hydrochloride) (RWJ 64809 hydrochloride) is a widely used p38 MAPK inhibitor.
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pan-Notch inhibitor
BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers. -
Notch inhibitor
Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer. -
pan-Akt inhibitor
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. -
PDE7/GSK3 inhibitor
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. -
BMP type I receptor inhibitor
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM). -
CK1 inhibitor
Epiblastin A is an inhibitor of Casein Kinase 1 (CK1) that engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs). -
GSK-3 inhibitor
GSK3 Inhibitor XIII (GSK3i XIII) is an ATP-binding site inhibitor of GSK-3. -
Notch Inhibitor
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity. -
ATP-competitive CK2 inhibitor
Ellagic acid hydrate is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM. -
BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β. -
YAP-TEAD Inhibitor
IAG933 is a potent YAP-TEAD inhibitor that targets the YAP/TAZ-TEAD interaction, demonstrating significant anti-tumor effects by promoting apoptosis in cancer cells. With an IC50 value of 9 nM against Avi-human TEAD4217-434, IAG933 serves as a valuable tool for studies investigating the YAP signaling pathway and its role in oncogenesis. Its oral bioavailability further enhances its utility in in vivo research applications focused on cancer therapeutics. -
YAP/TAZ Inhibitor
VT3989 is a potent YAP/TAZ inhibitor, targeting the essential Hippo signaling pathway regulators. It demonstrates significant inhibitory activity against firefly luciferase, with an IC50 value of less than 0.1 μM. This compound is ideal for research applications focused on understanding the roles of YAP/TAZ in cancer biology and cellular signaling pathways. -
pan-TEAD Inhibitor
GNE-7883 is a pan-TEAD inhibitor that disrupts the interaction between YAP/TAZ and TEAD transcription factors. This compound reduces chromatin accessibility at TEAD-binding sites and inhibits cell proliferation across various cell line models, demonstrating significant anti-tumor effects in vivo. Additionally, GNE-7883 addresses both intrinsic and acquired resistance to KRAS G12C inhibitors in multiple preclinical settings by targeting YAP/TAZ activation, making it a valuable tool for cancer research. -
Wnt/β-Catenin Inhibitor
MSAB is a potent and selective Wnt/β-catenin signaling inhibitor. By binding to β-catenin, it promotes its degradation and effectively downregulates Wnt/β-catenin target genes. MSAB demonstrates significant anti-tumor activity, particularly in Wnt-dependent cancer cell lines, making it a valuable tool for cancer research and therapeutic development targeting aberrant Wnt signaling. -
Dishevelled Protein PDZ Domain Inhibitor
3289-8625 is a potent inhibitor of the PDZ domain of Dishevelled (Dvl) protein, exhibiting a Kd of 10.6 μM. This compound effectively inhibits Wnt signaling pathways and demonstrates a significant impact on prostate cancer PC-3 cell growth, with an IC50 of 12.5 μM. 3289-8625 is valuable for research involving embryonic development and cancer biology. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
DKK1 Inhibitor
Gallocyanine chloride is a DKK1 inhibitor that targets the DKK1/LRP6 interaction, exhibiting an IC50 of 6.38 μM. This compound is relevant for research into Alzheimer's disease and related neurodegenerative tauopathies, as it activates the Wnt signaling pathway and promotes β-catenin accumulation. Additionally, Gallocyanine chloride demonstrates anti-metastatic, anti-inflammatory, and anti-fibrotic properties, and can serve as a fluorescent probe for the detection of superoxide anion radicals. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
SIRT Inhibitor
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity. -
δ-Secretase Inhibitor
δ-Secretase inhibitor 11 is a potent and selective inhibitor targeting δ-secretase, displaying an IC50 of 0.7 μM. This compound effectively interacts with both the active and allosteric sites of δ-secretase, resulting in the attenuation of tau and amyloid precursor protein cleavage. Its oral bioavailability and blood-brain barrier penetration make it suitable for in vivo studies, particularly in transgenic mouse models. δ-Secretase inhibitor 11 is a valuable tool for Alzheimer's disease research, facilitating investigations into the mechanisms underlying synaptic dysfunction and cognitive impairments. -
CK2 Inhibitor
CK2-TN03 is an ATP-competitive inhibitor of casein kinase 2 (CK2), demonstrating an IC50 of 165 nM and a Ki of 20 nM. This compound effectively inhibits CK2-mediated activation of survivin and reduces phosphorylation levels of critical proteins such as BRD4/MYCN and AKT1. CK2-TN03 has shown significant anti-neuroblastoma effects by promoting mitotic catastrophe and apoptosis in cancer cells, making it a valuable tool for research focused on neuroblastoma. -
p53 Activator/Wnt Inhibitor
PAWI-2 is a p53 activator and Wnt inhibitor that targets β3-KRAS signaling independently of KRAS. This compound selectively inhibits the phosphorylation of TBK1, resulting in the activation of apoptotic pathways, evidenced by increased caspase-3/7 activity and PARP cleavage. Additionally, PAWI-2 facilitates the translocation of optineurin into the nucleus and induces G2/M cell cycle arrest. It effectively reverses cancer stemness and overcomes drug resistance in integrin β3 KRAS-dependent human pancreatic cancer stem cells, demonstrating significant tumor growth inhibition in orthotopic xenograft mouse models.
