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Catalog No.
Product Name
Application
Product Information
Citations
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Allosteric Akt Inhibitor
MK-2206 free base is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8 nM, 12 nM, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer properties, particularly against breast cancer cell lines, as well as those harboring PIK3CA mutations and PTEN loss. MK-2206 free base is valuable for research applications focused on cancer biology and therapeutic development targeting the Akt pathway. -
Allosteric Akt Inhibitor
MK-2206 is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer activity, particularly in breast cancer cell lines and those harboring PIK3CA mutations or loss of PTEN function. MK-2206 is valuable for research investigating Akt's role in cancer progression and therapeutic resistance. -
Casein Kinase Inhibitor
Hematein is an allosteric inhibitor of casein kinase II, exhibiting an IC50 of 0.74 μM. It demonstrates significant biological activity by inhibiting Akt/PKB Ser129 phosphorylation and the Wnt/TCF signaling pathway. Research applications include studying apoptosis in lung cancer cells, making it a valuable reagent for cancer biology investigations. -
Wnt/β-catenin/NF-κB/AP-1 Inhibitor
Chikusetsusaponin IVa methyl ester is a natural triterpenoid saponin that functions as a Wnt/β-catenin, NF-κB, and AP-1 inhibitor. It induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells through the inhibition of the Wnt/β-catenin signaling pathway. Additionally, this compound significantly decreases the production of nitric oxide, prostaglandin E₂, and pro-inflammatory cytokines, while downregulating iNOS and COX-2 levels. Chikusetsusaponin IVa methyl ester is valuable for research focused on colorectal cancer and inflammatory processes. -
HDAC/CK2 Inhibitor
HDAC/CK2-IN-1 is an inhibitor targeting histone deacetylases HDAC1 and HDAC6, with IC50 values of 1.46 μM and 0.66 μM, respectively, as well as casein kinase 2 (CK2) with an IC50 of 3.67 μM. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including Jurkat, MCF-7, HCT-116, and HL-60. It serves as an important research tool for studying the roles of histone modifications and CK2 in tumor biology and could have potential implications in the development of cancer therapeutics. -
CK2/HDAC Inhibitor
IOR-160 is a dual inhibitor targeting casein kinase 2 (CK2) and histone deacetylases (HDACs). It showcases high selectivity for CK2, with an IC50 of 1.7 nM, and demonstrates broad inhibitory effects on HDACs 1, 2, 3, and 6, with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively. Through the inhibition of AKT phosphorylation and the enhancement of acetylated α-tubulin levels, IOR-160 effectively modulates critical cellular signaling pathways. This compound is particularly relevant in research focused on triple-negative breast cancer, where it has been shown to inhibit tumor growth and reduce tumor burden. -
HDACs Inhibitor
NL-103 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. This compound also targets the Hedgehog signaling pathway, leading to the downregulation of Gli2 expression. NL-103 is primarily utilized in cancer research, providing valuable insights into HDAC regulation and its role in tumor biology. -
HDAC6 Inhibitor
(S)-Trichostatin A is a selective inhibitor of HDAC6, demonstrating IC50 values of 9.88 nM and 11.1 nM for Zebrafish and Human HDAC6, respectively. It exhibits weak inhibition of other human HDACs, making it a valuable tool for studying HDAC6's role in cellular processes. This compound is useful in research applications related to cancer, neurodegenerative diseases, and epigenetic regulation. -
GSK-3β Inhibitor
Manzamine A hydrochloride is an orally active beta-carboline alkaloid that specifically inhibits GSK-3β and CDK-5, with IC50 values of 10.2 μM and 1.5 μM, respectively. This compound demonstrates significant antimalarial and anticancer properties, with additional effects such as inhibiting vacuolar ATPases and autophagy processes in pancreatic cancer cells. Furthermore, Manzamine A hydrochloride exhibits potent activity against HSV-1, making it valuable for various research applications in cancer biology and virology. -
PKG Inhibitor
Protein kinase G inhibitor-1 is a selective inhibitor targeting protein kinase G (PKG) with an IC50 of 0.9 μM. This compound is utilized primarily in research related to mycobacterial infections, providing insights into the mechanisms of pathogenesis and potential therapeutic approaches. Its efficacy in inhibiting PKG activity makes it a valuable tool for exploring mycobacterial biology and developing novel treatments. -
GSK-3β Inhibitor
GSK-3β inhibitor 13 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and GSK-3α, demonstrating IC50 values of 0.73 nM and 0.35 nM respectively. This orally active compound exhibits blood-brain barrier permeability and effectively reduces tau phosphorylation, with an IC50 of 58 nM. Its ability to modulate tau phosphorylation makes it valuable for research focused on neurodegenerative disorders, particularly Alzheimer's disease, by potentially mitigating the formation of neurofibrillary tangles. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 sodium is a selective inhibitor of WNT7A that disrupts the interaction between WNT7A and its receptor FZD5, leading to enhanced expression of MHC-I. This reagent is known to significantly increase levels of MHC-I and phosphorylated p65 while decreasing active β-catenin expression. Additionally, WNT7A-IN-1 sodium acts as a photosensitizer in the green spectral region, making it suitable for applications in photodynamic therapy and immunological studies. -
Hedgehog Inhibitor
Hedgehog IN-9 is a potent Hedgehog inhibitor that primarily targets the inhibition of GLI1 expression. It has been shown to enhance BRD2 protein levels in cells and effectively inhibit the growth of medulloblastoma spheroid cells. Additionally, Hedgehog IN-9 can be utilized for the synthesis of photoaffinity labeling probes, making it a valuable tool in cancer research and related biochemical applications. -
CDK/GSK3β/JNK Inhibitor
Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation. -
Wnt Inhibitor
Wnt Pathway Inhibitor 3 is a potent inhibitor of the Wnt signaling pathway, exhibiting an IC50 value of 45 nM. This compound demonstrates significant antiproliferative activity, making it a valuable tool for research in cancer biology and developmental studies. Its ability to modulate Wnt signaling can aid in the exploration of various cellular processes and disease mechanisms. -
Wnt Signaling Inhibitor
JW67 is a potent Wnt signaling inhibitor that targets the multiprotein complex composed of β-catenin, GSK-3β, AXIN, APC, and CK1, demonstrating an IC50 of 1.17 µM. By effectively reducing active β-catenin levels, JW67 leads to the downregulation of Wnt target genes, making it a valuable tool for studying Wnt signaling pathways. Additionally, JW67 inhibits the growth of colorectal cancer cells, providing potential applications in cancer research and therapeutic development. -
Wnt Inhibitor
Ipafricept is a recombinant fusion protein that functions as a Wnt inhibitor by binding to Wnt ligands via the extracellular portion of the human Frizzled-8 receptor fused with a human IgG1 Fc fragment. This mechanism effectively blocks Wnt signaling pathways, leading to reduced tumor growth and decreased liver and lung metastases when combined with Gemcitabine in pancreatic cancer mouse models. Additionally, Ipafricept demonstrates significant inhibitory activity against solid tumors, including desmoid tumor, germ cell cancer, and ovarian cancer, with an acceptable tolerance profile. -
Wnt Signaling Inhibitor
Coronaridine is an iboga alkaloid that functions as a Wnt signaling pathway inhibitor, effectively reducing β-catenin expression. This compound is primarily employed in research related to cancer biology, stem cell differentiation, and developmental processes, where dysregulation of the Wnt pathway is implicated. Its ability to modulate β-catenin levels makes it a valuable tool for investigating the mechanistic roles of Wnt signaling in various biological contexts. -
Wnt Inhibitor
WIC1 is a potent Wnt signaling inhibitor that targets the Wnt pathway, crucial for various biological processes, including cell proliferation and differentiation. This compound demonstrates significant anti-cancer activity by disrupting Wnt-mediated transcriptional activation, making it valuable for cancer research. WIC1 can be utilized in investigations of tumor growth, metastasis, and the overall role of Wnt signaling in oncogenesis. -
Wnt Inhibitor
Gigantol isomer-1 is a bibenzyl compound that functions as a Wnt inhibitor. This compound demonstrates significant therapeutic potential by targeting cancer cell proliferation and survival through modulation of the Wnt/β-catenin signaling pathway. Its capability to disrupt this crucial pathway makes it a valuable tool for research applications focused on cancer biology and therapeutic development. -
WNT1 Inhibitor
SJ26 is a potent Wnt1 inhibitor that exhibits anticancer activity. By targeting and inhibiting the expression of Wnt1, SJ26 disrupts Wnt1-mediated downstream signaling pathways, leading to a reduction in the migratory capacity of cancer cells. This compound is valuable for research focused on cancer progression and the role of Wnt signaling in tumor metastasis. -
Wnt/β-catenin Inhibitor
15-Oxospiramilactone is a diterpene derivative that functions as a Wnt/β-catenin signaling inhibitor. It exhibits significant biological activity by suppressing tumorigenesis in colon cancer cells, making it a valuable reagent for cancer research. This compound is suitable for studies investigating the modulation of the Wnt pathway and its implications in colorectal cancer progression. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 is a WNT7A inhibitor that disrupts the interaction between WNT7A and its receptor FZD5, leading to the upregulation of MHC-I expression. This compound enhances the expression of MHC-I and phosphorylated p65 while decreasing the levels of active β-catenin. Additionally, WNT7A-IN-1 serves as a photosensitizer in the green spectral region, making it valuable for research in cancer immunotherapy and photodynamic therapy applications. -
Wnt Pathway Inhibitor
Wnt Pathway Inhibitor 5 is a potent inhibitor of the Wnt signaling pathway, exhibiting an IC50 value of less than 0.003 µM. This compound demonstrates significant anti-cancer activity, making it effective against various malignancies such as ovarian teratocarcinoma, breast cancer, osteosarcoma, and head and neck squamous carcinoma. It serves as a valuable tool for researchers investigating the role of Wnt signaling in cancer progression and therapeutic interventions. -
Wnt/β-catenin Pathway Inhibitor
IWP-2-V2 is an analogue of IWP-2 that effectively inhibits the Wnt/β-catenin signaling pathway. This compound plays a significant role in modulating cellular processes related to development and cancer, making it a valuable tool for researchers studying the implications of Wnt signaling in various biological contexts. Its ability to disrupt β-catenin-mediated transcriptional activity positions IWP-2-V2 as a potential candidate for investigations into regenerative medicine and cancer therapy. -
Wnt Pathway Inhibitor
SEN461 is a potent and orally bioavailable inhibitor of the Wnt signaling pathway. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research applications in glioblastoma multiforme (GBM) and other cancers driven by aberrant Wnt pathway activation. Its efficacy in modulating Wnt-related processes highlights its potential for therapeutic development and mechanistic studies in cancer biology. -
Wnt/b-catenin Inhibitor
21H7 is a selective inhibitor of the Wnt/β-catenin signaling pathway. This compound significantly inhibits cell proliferation in hair follicles and demonstrates potent growth suppression of breast and colon cancer cells. Due to its specific targeting of the Wnt/β-catenin pathway, 21H7 serves as a valuable tool in cancer research and therapeutic development. -
β-Catenin Inhibitor
β-Catenin-IN-7 is an inhibitor of β-catenin, specifically disrupting the interaction between β-catenin and Tcf-4. This compound effectively inhibits Wnt-dependent target gene expression, demonstrating significant anti-cancer activity. It is a valuable tool for research applications focused on cancer biology and the Wnt signaling pathway. -
Wnt Signal Inhibitor
Wnt/β-catenin-IN-7 is a Wnt signaling pathway inhibitor with an IC50 of 0.15 μM. This compound effectively disrupts β-catenin-mediated transcriptional activation, making it valuable for investigating the role of Wnt signaling in cancer and fibrosis. Its potent inhibitory activity supports research into therapeutic targets within these pathological conditions. -
β-catenin Inhibitor
PMED-1 is a potent β-catenin inhibitor that effectively diminishes β-catenin activity in hepatoblastoma and various hepatocellular carcinoma (HCC) cell lines, exhibiting an IC50 range of 4.87 to 32 μM. This compound disrupts Wnt signaling by reducing the interaction between β-catenin and CREB binding protein, leading to the inhibition of cell proliferation. PMED-1 is a valuable tool for cancer research, particularly in studies focused on targeting aberrant Wnt signaling pathways. -
Wnt/β-catenin Inhibitor
Wnt/β-catenin-IN-4 is a potent inhibitor of the Wnt/β-catenin signaling pathway. This compound effectively disrupts β-catenin-dependent transcription, making it a valuable tool for investigating the role of Wnt signaling in various biological processes. It is commonly utilized in cancer research, developmental biology, and studies related to stem cell differentiation. -
Hedgehog Inhibitor
Hh Pathway-IN-1 is a potent inhibitor of the Hedgehog (Hh) signaling pathway, acting primarily as a Gli antagonist. With an IC50 value of 1.1 µM in C3H10T1/2 cells, it demonstrates significant inhibition of Hh pathway functionality while sparing Wnt signaling. Hh Pathway-IN-1 exhibits anti-proliferative effects and reduces GLI1 mRNA expression, contributing to its efficacy in inhibiting colony formation in a dose-dependent manner. This compound is valuable for research in developmental biology and cancer therapeutics targeting the Hedgehog pathway. -
Hedgehog Pathway Inhibitor
3-epi-Vitamin D3, also known as Epicholecalciferol, functions as a Hedgehog pathway inhibitor, exhibiting an IC50 value of 39.2 μM in U87MG cell lines. This Vitamin D3 analogue is useful in studies investigating the modulation of the Hedgehog signaling pathway, which plays a critical role in cellular growth and differentiation. 3-epi-Vitamin D3 may have potential applications in cancer research, particularly in contexts where Hedgehog dysregulation is implicated. -
Hedgehog Inhibitor
Hedgehog IN-1 is a potent inhibitor of the Hedgehog signaling pathway, demonstrating an IC50 of 70 nM. This compound effectively blocks Hedgehog protein activity, making it valuable for research into developmental biology and cancer therapeutics. Hedgehog IN-1 is instrumental in studies aimed at understanding the role of the Hedgehog pathway in tumorigenesis and potential therapeutic applications in related disorders. -
Hh Pathway Inhibitor
T-1330 is an inhibitor of the Hedgehog (Hh) signaling pathway, specifically targeting the downstream effector Gli1. By effectively reducing Gli1 expression, T-1330 plays a crucial role in modulating Hh pathway activity. This compound is useful in research applications related to developmental biology and cancer therapy, particularly in studies investigating aberrant Hh signaling in various malignancies. -
Hedgehog Pathway Inhibitor
Hedgehog IN-2 is a potent inhibitor of the Hedgehog signaling pathway, exhibiting an IC50 value of less than 0.003 μM in C3H10T1/2 cells. This compound effectively disrupts Hedgehog-mediated cellular signaling, making it a valuable tool for studying embryonic development, cancer biology, and regenerative medicine. Its high potency and specificity enable researchers to investigate the role of the Hedgehog pathway in various biological processes and disease states. -
Hedgehog Inhibitor
Hedgehog IN-6 is a potent Hedgehog (Hh) inhibitor that targets the Hh signaling pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo). By obstructing the cholesterization of Smo, Hedgehog IN-6 effectively inhibits Hh pathway activation, which is crucial in various cancer types. This compound is valuable for research applications aimed at understanding and manipulating Hh signaling in oncogenesis and developmental biology. -
Hedgehog Pathway Inhibitor
HPP-9 is a Hedgehog Pathway inhibitor designed as a Proteolysis-Targeting Chimera (PROTAC) that effectively degrades BET bromodomains. With a pIC50 of 6.71, HPP-9 exhibits significant antitumor activity. This compound is valuable for research applications focused on cancer biology and the modulation of the Hedgehog signaling pathway. -
Hedgehog Pathway Inhibitor
Hedgehog IN-3 is a potent inhibitor of the Hedgehog signaling pathway, exhibiting an IC50 of 0.01 µM. This compound is primarily utilized in cancer research to investigate the role of Hedgehog-mediated signaling in tumorigenesis and cellular proliferation. Its effectiveness in modulating this pathway makes it a valuable tool for studying various malignancies and developing targeted therapeutic strategies. -
Hedgehog Inhibitor
Hedgehog IN-10 is a potent inhibitor of the Hedgehog signaling pathway, targeting essential components in cellular signaling. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate Hedgehog signaling contributes to investigations into therapeutic strategies for tumors associated with dysregulated Hedgehog pathway activity. -
Hh Inhibitor
Physalin H is a bioactive compound extracted from Solanum nigrum, functioning as a Hedgehog (Hh) signaling inhibitor. It effectively disrupts GLI1-DNA complex formation and inhibits GLI1 transcription with an IC50 of 0.7 μM. Additionally, Physalin H exhibits cytotoxic effects on PANC1 and DU145 cancer cell lines, demonstrating IC50 values of 5.7 μM and 6.8 μM, respectively. This compound is valuable for research into Hh pathway modulation and cancer therapeutics. -
Hedgehog Pathway Inhibitor
Hedgehog IN-5 is a small molecule inhibitor that targets the Hedgehog signaling pathway. This orally active compound is primarily employed in research pertaining to fibrotic diseases, providing valuable insights into the mechanisms underlying this condition. Its ability to modulate Hedgehog pathway activity makes it a significant tool for exploring therapeutic strategies in related biological contexts. -
Hedgehog Inhibitor
Hedgehog IN-4 is a potent inhibitor of the Hedgehog signaling pathway, acting as a benzamide derivative with an IC50 of 0.050 nM. It effectively disrupts Hedgehog-mediated cellular processes, making it valuable for research on developmental biology, cancer, and regenerative medicine. Its ability to modulate this critical pathway allows for exploration into the mechanisms of diseases associated with Hedgehog signaling dysregulation. -
YAP/TEAD Inhibitor
YAP/TEAD-IN-2 is a potent inhibitor of the YAP/TEAD protein complex. It effectively reduces luciferase activity driven by YAP/TEAD in 293T cells, demonstrating its function as a reliable research tool. Additionally, YAP/TEAD-IN-2 exhibits significant anti-proliferative effects against human pleural mesothelioma NCI-H226 cells. This compound is relevant for research exploring diseases related to dysregulation of the Hippo signaling pathway, particularly in the context of various cancer types. -
YAP1/TAZ-TEAD Inhibitor
K-975 is a selective and orally bioavailable TEAD inhibitor that disrupts protein-protein interactions between YAP1/TAZ and TEAD. This compound forms a covalent bond with Cys359 within the palmitate-binding pocket of TEAD through its acrylamide structure. K-975 demonstrates significant antitumor activity, particularly in the treatment of malignant pleural mesothelioma, making it a valuable tool for cancer research and therapeutic investigations targeting the YAP1/TAZ-TEAD signaling pathway. -
YAP/TAZ Inhibitor
VT104 is a potent and orally active inhibitor of the YAP/TAZ signaling pathway. It effectively prevents the palmitoylation of endogenous TEAD1 and TEAD3 proteins, thereby modulating downstream gene expression. This compound is valuable for research applications focused on cancer biology, particularly in studies aimed at understanding the role of YAP/TAZ in oncogenesis and tumor progression. -
YAP-TEAD Inhibitor
TED-347 is a potent irreversible allosteric inhibitor of the YAP-TEAD protein-protein interaction, exhibiting an EC50 of 5.9 μM for the TEAD4-Yap1 complex. The compound covalently binds to Cys-367 within the central pocket of TEAD4, with a Ki value of 10.3 μM. By inhibiting TEAD transcriptional activity, TED-347 demonstrates significant antitumor potential, making it a valuable tool for cancer research and therapeutic studies focused on the Hippo signaling pathway. -
YAP/TAZ-TEAD Inhibitor
SWTX-143 is an orally active inhibitor of the YAP/TAZ-TEAD signaling pathway, targeting the palmitoylation pocket across all four TEAD isoforms. This compound demonstrates irreversible and selective suppression of YAP/TAZ-TEAD transcriptional activity, highlighting its potential in antitumor research. SWTX-143 serves as a valuable tool for investigating the mechanistic roles of YAP/TAZ-TEAD in oncogenesis and therapeutic strategies against cancer. -
TEAD-YAP/TAZ Inhibitor
YAP/TAZ Inhibitor-2 is a potent and orally bioactive compound that targets the TEAD-YAP/TAZ signaling pathway, demonstrating an EC50 of 3 nM. This inhibitor exhibits significant anti-proliferative effects, making it a valuable tool for research into tumorigenesis and cancer biology. Its antitumor activity further supports its application in studies focused on cellular proliferation and tumor growth regulation. -
YAP/TAZ-TEAD Inhibitor
MSC-4106 is a potent, orally active inhibitor targeting the YAP/TAZ-TEAD signaling pathway. This compound effectively inhibits the auto-palmitoylation of TEAD1 and TEAD3, demonstrating significant biological activity. MSC-4106 has been shown to exert inhibitory effects in the NCI-H226 tumor xenograft model, making it a valuable tool for cancer research and therapeutic development.
