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Catalog No.
Product Name
Application
Product Information
Citations
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MDM2 Inhibitor
Caylin-1 is a potent inhibitor of MDM2, functioning through direct binding to the protein to disrupt its interaction with p53. This compound is an analog of Nutlin-3 and exhibits additional binding affinity to Bcl-XL, making it a valuable tool in multi-target anticancer research. Caylin-1's unique properties facilitate investigations into oncogenic pathways and the therapeutic potential of cancer treatments targeting both MDM2 and Bcl-XL. -
DNAJA1-mutP53 R175H Inhibitor
GY1-22 is an inhibitor targeting the DNAJA1-mutP53 R175H interaction pocket. This compound exhibits significant biological activity in disrupting the function of mutant p53, an important factor in various cancer types. GY1-22 is suitable for cancer research applications, particularly in studies focused on p53 mutations and their implications in tumorigenesis. -
MDM-2/p53 Inhibitor
AM-8553 is a potent MDM2/p53 inhibitor, exhibiting a binding affinity with a KD of 0.4 nM for MDM2. This compound demonstrates significant anti-tumor activity by disrupting the MDM2-p53 interaction, thereby stabilizing p53 and promoting its tumor suppressive functions. AM-8553 is applicable in cancer research, particularly in studies targeting the MDM2/p53 pathway for therapeutic interventions. -
MDM2 Inhibitor
TB114 is a selective inhibitor of the MDM2 protein, demonstrating a Ki value of 0.4 nM. By inhibiting MDM2, TB114 enhances the tumor-suppressive functions of p53, leading to increased apoptosis in cancer cells. This compound holds significant promise for research applications focused on cancer therapies that target the MDM2-p53 interaction. -
MDM2 Inhibitor
Siremadlin succinate is a potent MDM2 inhibitor that selectively targets the p53-binding pocket of MDM2, disrupting its ability to mediate the ubiquitination and degradation of the p53 tumor suppressor. By activating the p53 pathway, Siremadlin succinate promotes p53-dependent cell cycle arrest and apoptosis in p53 wild-type cells. This compound is valuable for research applications focused on cutaneous melanoma and other cancers with dysregulated p53 signaling. -
S100A2-p53 Interaction Inhibitor
S100A2-p53-IN-1 is a specific inhibitor of the S100A2-p53 protein interaction. S100A2, a calcium-binding protein, plays a significant role in cell signaling and is upregulated in pancreatic cancer. This compound demonstrates potent inhibitory activity against the MiaPaCa-2 pancreatic cancer cell line, achieving a growth inhibition concentration (GI50) in the range of 1.2-3.4 μM. It serves as a valuable tool for investigating the S100A2-p53 pathway in cancer research. -
TP53-MDM2 Inhibitor
NVP-CFC218 is a selective inhibitor targeting the TP53-MDM2 interaction, effectively displacing the p53 peptide from HDM2 with an IC50 value of 1.6 nM. This compound is instrumental in assessing pharmacological sensitivity in various cell line models and is widely utilized in cancer research to study tumor suppressor pathways and MDM2-mediated p53 regulation. -
MDM2/p53 Inhibitor
Phage-derived 12/1 peptide is a potent inhibitor of the MDM2/p53 interaction, effectively disrupting the binding between MDM2 and p53, as well as MDMX and p53. This peptide demonstrates significant antitumor activity, exhibiting IC50 values of 0.15 μM for MDM2 and 1.25 μM for MDMX. It serves as a valuable tool for research investigating the modulation of p53 activity and the therapeutic potential in targeting MDM2/MDMX pathways in cancer. -
MDM2/MDMX-p53 Interaction Inhibitor
pDI is a synthetic peptide that functions as an inhibitor of the MDM2 and MDMX-p53 interactions, exhibiting half-maximal inhibitory concentrations (IC50) of 10 nM and 100 nM, respectively. This compound is essential for research focused on colorectal cancer, providing insights into tumor suppression mechanisms and the modulation of p53 activity. Its ability to disrupt these critical protein-protein interactions makes pDI a valuable tool in cancer therapeutic studies. -
p53-MDM2 Inhibitor
p53-MDM2-IN-2 is an orally active inhibitor targeting the p53-MDM2 interaction, exhibiting a Ki value of 0.25 μM. This compound demonstrates antitumor activity through the inhibition of the NF-κB signaling pathway. It is valuable in research studies focusing on cancer therapy and elucidating the molecular mechanisms of tumor suppression. -
MDM2 Inhibitor
MI-1063 is a selective inhibitor of MDM2 that disrupts the MDM2-p53 interaction, thereby activating the tumor suppressor activity of p53. This compound effectively inhibits the proliferation of cancer cell lines RS4-11 and MV4-11, demonstrating IC50 values of 179 nM and 93 nM, respectively. Additionally, MI-1063 serves as a valuable target protein ligand in the synthesis of the PROTAC degrader MD-265, facilitating advancements in targeted protein degradation research. -
MDM2 Inhibitor
MDM2-IN-26 is an inhibitor targeting MDM2, a critical negative regulator of the tumor suppressor p53. By disrupting the MDM2-p53 interaction, this compound effectively activates p53's tumor suppressor functions, providing a promising approach for cancer research. MDM2-IN-26 can be utilized to study the modulation of p53 activity in various cancer models and therapeutic applications. -
p53-MDM2 Inhibitor
p53-MDM2-IN-3 is a potent p53-MDM2 inhibitor with a Ki value of 0.25 μM, demonstrating oral bioavailability. This compound exhibits significant antitumor activity through its inhibition of the NF-κB signaling pathway. It serves as a valuable tool for cancer research, particularly in studies focused on targeting the p53-MDM2 interaction and the subsequent effects on tumor proliferation and survival. -
MDM2-p53 Inhibitor
MDM2-p53-IN-18 is a potent inhibitor of the MDM2-p53 protein-protein interaction. This compound effectively disrupts the binding of MDM2 to the tumor suppressor p53, leading to the stabilization and activation of p53. It demonstrates significant biological activity in promoting apoptosis and cell cycle arrest in cancer cells, making it valuable for research applications in oncology and drug discovery targeting p53-related pathways. -
MDM2-p53 Inhibitor
Nutlin-2 is a selective inhibitor of the interaction between MDM2 and p53, exhibiting an IC50 of 0.14 μM. By occupying the hydrophobic pocket of MDM2, Nutlin-2 effectively disrupts the protein-protein interaction crucial for the regulation of p53, allowing for the stabilization and activation of this tumor suppressor. This compound is primarily utilized in cancer research to study p53-mediated pathways and to explore therapeutic avenues in tumors with MDM2 overexpression. -
MDM2 Inhibitor
RO5353 is an orally active MDM2 inhibitor that effectively disrupts the p53-MDM2 interaction, with an IC50 of 7 nM for MDM2. It demonstrates potent inhibitory effects on the proliferation of wild-type p53 cancer cells, achieving an average IC50 of 7 nM. In vivo studies reveal that RO5353 possesses significant antitumor efficacy and favorable pharmacokinetic properties in murine models, making it a valuable tool for cancer research focused on p53 pathway modulation. -
MDM-2/p53 Inhibitor
MDM2-p53-IN-20 is a synthetic inhibitor targeting the MDM2-p53 protein interaction. This compound disrupts the binding of MDM2 to p53, promoting the stabilization and activation of p53, a critical tumor suppressor involved in cell cycle regulation and apoptosis. MDM2-p53-IN-20 is primarily utilized in cancer research to study p53 pathway activation and to explore therapeutic strategies for tumors exhibiting MDM2 overexpression. -
PKC/PKD Inhibitor
PKC/PKD-IN-1 is a potent dual inhibitor of protein kinase C and protein kinase D, exhibiting an IC50 of 0.6 nM against PKD1. This compound demonstrates the ability to mitigate cardiac hypertrophy induced by high-salt diets, making it a valuable tool for investigating mechanisms related to heart failure. Its specificity and efficacy position it as a significant reagent for researchers focused on cardiac disease and kinase signaling pathways. -
PKD Inhibitor
3-IN-PP1 is a selective inhibitor of protein kinase D (PKD), demonstrating potent inhibition across PKD isoforms PKD1, PKD2, and PKD3 with IC50 values of 108 nM, 94 nM, and 108 nM, respectively. This compound exhibits broad-spectrum anticancer activity, effectively inhibiting the proliferation of various tumor cell lines. 3-IN-PP1 serves as a valuable tool for cancer research, particularly in studying the role of PKD signaling pathways in tumor growth and development. -
PKD Inhibitor
Protein kinase D inhibitor 1 is a potent pan-PKD inhibitor that exhibits IC50 values between 17 to 35 nM. This compound selectively inhibits the phosphorylation of cortactin mediated by Protein kinase D, thereby influencing cellular processes related to cytoskeletal dynamics and signal transduction. It is valuable for research applications focused on studying PKD signaling pathways and their impact on various cellular functions. -
RIPK2/3 Inhibitor
RIPK2/3-IN-2 is a potent dual inhibitor of receptor-interacting protein kinases 2 and 3 (RIPK2 and RIPK3), exhibiting IC50 values of 12 nM and 18 nM, respectively. This compound effectively induces necroptosis, showcasing an EC50 value of 0.16 μM. RIPK2/3-IN-2 can be utilized in research exploring programmed cell death mechanisms and the role of necroptosis in various pathological conditions. -
Cell-cycle Inhibitor, Senescence Inducer, Apoptosis Inducer, Antiproliferative Agent
Anticancer agent 299 is a cell-cycle inhibitor that functions as a senescence and apoptosis inducer, exhibiting significant antiproliferative effects on cancer cells. This compound demonstrates selective cytotoxicity against cancerous cells with minimal impact on non-tumoral chondrocyte cells at therapeutic concentrations. Anticancer agent 299 is particularly useful for research related to ER+/HER2− breast cancer and BRAF-mutant melanoma. -
MIF Inhibitor
MIF-IN-1 is a potent inhibitor of macrophage migration inhibitory factor (MIF), with a reported pIC50 of 6.87. This compound is designed to selectively inhibit MIF activity, which plays a critical role in various inflammatory and immune responses. MIF-IN-1 is suitable for research applications focused on inflammation, autoimmune diseases, and cancer biology, providing valuable insights into MIF-mediated pathways. -
D-DT Inhibitor
RGB097 is a potent inhibitor of D-dopachrome tautomerase (D-DT), demonstrating an IC50 value of 0.5 µM. This compound exhibits significant biological activity and has potential applications in cancer research, particularly in elucidating the role of D-DT in oncogenesis and tumor progression. -
MIF Inhibitor
MIF-IN-5 is a potent and reversible inhibitor of macrophage migration inhibitory factor (MIF), exhibiting a competitive mechanism of action. With an IC50 of 4.8 μM and a Ki value of 3.3 μM, it effectively disrupts MIF's biological activity. This compound is valuable for research applications involving inflammation, immune response modulation, and potential therapeutic strategies targeting various diseases associated with MIF dysregulation. -
MIF Inhibitor
HTS05585 is a selective inhibitor of macrophage migration inhibitory factor (MIF), demonstrating a Kd value of 0.29 μM via microscale thermophoresis and 0.32±0.01 μM confirmed by isothermal titration calorimetry. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-6, and IL-1β, from LPS-stimulated macrophages. HTS05585 is a valuable tool for studying inflammation-related diseases, particularly in the context of sepsis research. -
MIF tautomerase Inhibitor
TE-11 is a potent MIF tautomerase inhibitor, exhibiting an IC50 value of 5.63 μM. This compound effectively ameliorates CD-like colitis and reduces migration of MIF-induced eosinophils and neutrophils. Additionally, TE-11 prevents M1 polarization and the associated metabolic reprogramming, making it a valuable tool for research in inflammatory and autoimmune disorders. -
PERK Inhibitor
PERK-IN-2 is a highly potent inhibitor of the PERK (PKR-like ER kinase) pathway, exhibiting an IC50 of 0.2 nM. This compound effectively modulates unfolded protein response (UPR) signaling, making it valuable for studies investigating the roles of PERK in cellular stress responses and related diseases. Applications include research on cancer biology, neurodegeneration, and metabolic disorders. -
PERK Inhibitor
PERK-IN-4 is a highly selective inhibitor of the protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), demonstrating an IC50 of 0.3 nM. This compound effectively modulates the PERK pathway, which is activated in response to various endoplasmic reticulum stresses associated with numerous disease states. PERK-IN-4 is valuable for research applications focused on cellular stress responses and potential therapeutic strategies in diseases linked to the unfolded protein response. -
PERK Inhibitor
HC-5404-Fu is a potent and orally active inhibitor of the protein kinase PERK, exhibiting an IC50 of 0.001 μM against human PERK. By blocking PERK activation induced by VEGFR-TKIs, HC-5404-Fu disrupts the adaptive stress response that typically enhances tumor survival. This compound enhances anti-angiogenic effects by inhibiting the formation of both newly formed and mature tumor blood vessels, particularly in renal cell carcinoma models. HC-5404-Fu is suitable for research focused on tumor biology and angiogenesis in renal cell carcinoma. -
PERK Inhibitor
PERK-IN-5 is a highly potent inhibitor of PERK (Protein kinase RNA-like endoplasmic reticulum kinase), demonstrating IC50 values of 2 nM and 9 nM for PERK and phosphorylated eIF2α, respectively. This compound is selectively and orally bioavailable, making it an advantageous tool for in vivo studies. PERK-IN-5 has been shown to significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft model, positioning it as a valuable reagent for cancer research focusing on the UPR (unfolded protein response) pathway. -
PERK Inhibitor
(S)-PERK-IN-5 is a selective inhibitor of the protein kinase PERK (PKR-like endoplasmic reticulum kinase), exhibiting an IC50 range of 0.101-0.250 μM. This compound plays a critical role in studies focused on the unfolded protein response and endoplasmic reticulum stress pathways. Its application is pertinent in exploring therapeutic strategies for diseases associated with protein misfolding and metabolic dysregulation. -
PERK Inhibitor
PERK-IN-3 is a highly selective inhibitor of the Protein Kinase R (PKR)-like ER kinase (PERK) with an IC50 value of 7.4 nM. This compound effectively modulates the unfolded protein response, promoting cell survival under ER stress. It is primarily utilized in research investigating the role of PERK in cellular stress pathways, cancer biology, and neurodegenerative diseases. -
PERK Inhibitor
PERK-IN-6 is a selective inhibitor of the Protein Kinase RNA-like Endoplasmic Reticulum Kinase (PERK), exhibiting an IC50 value of 2.5 nM. This compound inhibits PERK-mediated signaling pathways, making it a valuable tool for investigating the role of ER stress and unfolded protein response in various cellular processes. PERK-IN-6 is suitable for research applications in studying diseases associated with dysregulated PERK activity, including neurodegeneration and cancer. -
MIF Inhibitor
4-IPP (4-Iodo-6-phenylpyrimidine) is a selective suicide substrate and irreversible inhibitor targeting macrophage migration inhibitory factor (MIF). This compound significantly impedes MIF activity, making it a valuable tool for research into inflammatory processes, cancer progression, and immune response modulation. Its ability to inhibit MIF provides insights into the underlying mechanisms of various pathologies, facilitating the development of therapeutic strategies. -
MIF Inhibitor
ISO-92 is a selective inhibitor of migration inhibitory factor (MIF) with an IC50 of 550 nM. This compound effectively reduces inflammatory activity and demonstrates a dose-dependent inhibition of hypoxia-induced proliferation in the CCL-210 cell line. In mouse models of hypoxia, ISO-92 significantly decreases the thickness of the pulmonary vascular wall. Its unique mechanism makes ISO-92 a valuable tool for investigating inflammatory and neurological disorders. -
MIF-2 Inhibitor
4-CPPC is a potent and selective inhibitor of Macrophage Migration Inhibitory Factor 2 (MIF-2), demonstrating a Ki value of 33 µM. This compound exhibits reversible inhibition, showcasing a notable selectivity over MIF-1 with a Ki value of 431 µM. 4-CPPC is valuable for research applications aimed at elucidating the role of MIF-2 in inflammatory responses and other pathological conditions, making it a critical tool for studying MIF-related signaling pathways. -
MIF Inhibitor
RDR 03785 is a covalent inhibitor of Macrophage Migration Inhibitory Factor (MIF), exhibiting an IC50 of 0.36 μM. This compound demonstrates significant biological activity in modulating MIF-related pathways, making it a valuable tool in the study of inflammatory diseases and immune response regulation. Research applications include exploring MIF's role in various pathophysiological processes, as well as potential therapeutic interventions targeting MIF. -
MIF Inhibitor
MKA031 is a non-competitive inhibitor of macrophage migration inhibitory factor (MIF) with an IC50 value of 1.7 μM. This compound disrupts the interaction between MIF and AIF, impedes MIF nuclear translocation, and interferes with N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced cell death. MKA031 is particularly useful for research applications focused on chronic hepatitis C virus infection and related cellular pathways. -
MIF2 Tautomerase Inhibitor
R110 is a potent competitive inhibitor of macrophage migration inhibitory factor 2 (MIF2) tautomerase, exhibiting an IC50 of 15 μM. This compound is valuable for research into cancer biology, specifically in mechanisms related to tumor progression and immune modulation. By targeting MIF2, R110 offers potential insights into therapeutic strategies for cancer treatment. -
MIF2 Tautomerase Inhibitor
MIF2-IN-1 is a potent inhibitor of the MIF2 tautomerase, exhibiting an IC50 of 1.0 μM. This compound effectively suppresses the proliferation of non-small cell lung cancer cells by inducing cell cycle arrest through the deactivation of the MAPK signaling pathway. MIF2-IN-1 is a valuable tool for researching cancer biology and therapeutic strategies in oncology. -
MIF Inhibitor
MIF-IN-4 hydrochloride is a potent inhibitor of macrophage migration inhibitory factor (MIF), with an affinity corresponding to a pIC50 of 5.01-6. MIF is a crucial cytokine involved in regulating macrophage migration and immune responses. This compound is valuable for research applications focused on inflammation, immune modulation, and related pathways. -
MIF Inhibitor
MIF-IN-6 is a potent inhibitor of macrophage migration inhibitory factor (MIF), exhibiting an IC50 of 1.4 μM and a Ki value of 0.96 μM. This compound effectively attenuates MIF-induced ERK phosphorylation and inhibits the proliferation of A549 cells, making it valuable for studies related to cancer biology and inflammation. Its mechanism of action positions MIF-IN-6 as a significant tool for exploring MIF-related pathways and potential therapeutic interventions. -
NF-κB Inhibitor, GPx Inhibitor, HIV Replication Inhibitor
α-MSH (11-13) acetate is a selective melanocortin-1 receptor ligand that functions as an inhibitor of NF-κB, GPx activity, and HIV replication. It induces an acute elevation of intracellular calcium levels under certain costimulation or pathway inhibition conditions. This compound effectively suppresses TNF-α-induced NF-κB activation, inhibits colony formation of Staphylococcus aureus and Candida albicans, and demonstrates potential in the study of infections related to these pathogens, as well as in traumatic brain injury, corneal epithelial wounds, and inflammatory bowel disease research. -
PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
p53 inhibitor
inhibits p53 binding to mitochondria by reducing its affinity for antiapoptotic proteins Bcl-2 and Bcl-XL. -
p53 inhibitor
Pifithrin-α hydrobromide is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression.
