Catalog No.
Product Name
Application
Product Information
Citations
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p53-MDM2 Inhibitor
p53-MDM2-IN-5 is a potent inhibitor of the p53-MDM2 interaction. This compound induces apoptosis, promotes autophagy, and causes DNA damage in cells, contributing to its anti-tumor efficacy. Additionally, p53-MDM2-IN-5 effectively induces cell cycle arrest at both the S and G2/M phases, making it a valuable tool for cancer research applications focused on therapeutic strategies targeting the p53 pathway. -
MDM2-p53 Interaction Inhibitor
MI-773 TFA is a selective inhibitor of the MDM2-p53 interaction, demonstrating a Ki of 0.88 nM for MDM2. By disrupting the MDM2-TP53 interaction, MI-773 TFA effectively activates the p53 tumor suppressor pathway, leading to apoptotic cell death. This compound has shown significant anticancer activity, inducing tumor regression in xenograft models of adenoid cystic carcinoma and exhibiting therapeutic potential in neuroblastoma. MI-773 TFA serves as a valuable tool for research focused on p53-related cancer therapies. -
MDM2/MDMX Inhibitor
MDMX/MDM2-IN-2 is a potent dual inhibitor of the p53-MDM2/MDMX interaction, exhibiting inhibition constants (Kis) of 0.23 µM for MDM2 and 2.45 µM for MDMX. This compound effectively disrupts the binding of p53 to MDM2 and MDMX, thereby restoring p53's function, which leads to cell cycle arrest and apoptosis. Additionally, MDMX/MDM2-IN-2 demonstrates inhibition of cell migration and invasion, highlighting its potential for therapeutic applications in cancer research. Its antitumor activity makes it a valuable tool for studying tumor biology and exploring novel cancer treatment strategies. -
MDM2 Inhibitor
D-CopA3 functions as an MDM2 inhibitor, promoting the activation of the p53 signaling pathway. It demonstrates significant cytotoxicity against colorectal cancer cell lines HCT-116, LoVo, and RKO, with an IC50 ranging from 15 to 18 μM, and induces JNK/Beclin-1-mediated autophagy. Additionally, D-CopA3 reduces the expression of the cell cycle inhibitor p21Cip1/Waf1, enhances mucosal barrier function, and exhibits anti-inflammatory properties in models of acute enteritis and chronic colitis. Furthermore, it has shown anti-tumor efficacy in HCT-116 mouse xenograft models. -
MDM-2/p53 MDM2 Inhibitor
CTX1 is a selective inhibitor of MDM2, designed to alleviate HdmX-mediated repression of the tumor suppressor protein p53. This compound demonstrates significant anti-cancer activity, particularly in mouse models of acute myeloid leukemia (AML). CTX1 is utilized in research focused on cancer therapeutics and the modulation of p53 pathways. -
MDM-2/p53 MDM2 Inhibitor
p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a selective inhibitor of the interaction between the tumor suppressor protein p53 and its negative regulator MDM2. This compound enhances p53 activity, highlighting its potential as an anticancer agent by promoting apoptosis in p53-deficient tumors. It is valuable for research applications focused on cancer therapy, cell cycle regulation, and the molecular mechanisms of tumorigenesis. -
p53-MDM2/X Inhibitor
p53-MDM2-IN-4 is a potent inhibitor of the p53-MDM2/X protein interaction, displaying a Ki value of 3.079 μM. This compound effectively disrupts the MDM2-mediated inhibition of p53, promoting the stabilization and activation of the tumor suppressor protein. p53-MDM2-IN-4 holds significant potential in anti-tumor research and therapeutic development targeting cancer's reliance on the p53 pathway. -
p53-MDM2/X Inhibitor
p53-MDM2-IN-1 is an inhibitor of the p53-MDM2/X protein interaction, exhibiting a Ki value of 23.35 µM. This compound is valuable for anti-tumor research, as it disrupts the interaction between p53 and MDM2/X, potentially restoring p53 function in cancer cells. Its application can enhance the understanding of tumor biology and contribute to the development of novel therapeutic strategies targeting this pathway. -
MDM-2/p53 MDM2 Inhibitor
NVP-CGM097 sulfate is a selective inhibitor of the MDM2-p53 interaction, demonstrating an IC50 of 1.7±0.1 nM for human MDM2. This compound effectively disrupts the MDM2-mediated suppression of p53, leading to the activation of p53-dependent pathways. NVP-CGM097 sulfate is utilized in research focused on cancer therapeutics and the modulation of tumor suppressor activities. -
p53-MDM2 Binding Inhibitor
NU-8231 is a potent inhibitor of the p53-MDM2 interaction, exhibiting an IC50 range of 5.3-200 μM. This compound is instrumental in cancer research, facilitating studies on the restoration of p53 function and the modulation of apoptotic pathways. Its ability to disrupt the p53-MDM2 binding offers potential insights into therapeutic strategies targeting p53-mediated tumor suppression. -
MDM2 Inhibitor
AM-6761 is a highly potent inhibitor of MDM2, exhibiting an IC50 of 0.1 nM. This compound is crucial for studies on cancer biology, particularly in understanding the regulatory mechanisms of p53 and its interactions with MDM2. AM-6761 is primarily used in cancer research to evaluate potential therapeutic strategies targeting MDM2-mediated pathways. -
MDM-2/p53 MDM2 Inhibitor
AM-8735 is a selective inhibitor of the MDM2 protein, targeting its interaction with the p53 tumor suppressor. It exhibits potent activity with an IC50 of 25 nM, making it a valuable tool for cancer research. This compound is utilized in studies investigating the reactivation of p53 in tumor models, offering potential insights into therapeutic strategies for p53-deficient cancers. -
MDM2/XIAP Inhibitor
MDM2/XIAP-IN-1 is a potent inhibitor of both MDM2 and XIAP, exhibiting significant anti-cancer activity with an IC50 value of 0.3 μM. This compound is suitable for use in cancer research, facilitating studies aimed at dissecting the role of MDM2 and XIAP in tumor progression and survival. Its dual-targeting mechanism allows for exploration of therapeutic strategies that may enhance apoptosis in cancer cells. -
MDM2 Inhibitor
SP-141 is a selective inhibitor of MDM2, a protein that regulates the p53 tumor suppressor pathway. By promoting MDM2 auto-ubiquitination and subsequent degradation, SP-141 enhances p53 activity, which can lead to increased cell cycle arrest and apoptosis. This compound is a valuable tool for investigating therapeutic strategies in pancreatic and breast cancer research. -
MDM2 Ligand
MDM2 Ligand 5 is a potent ligand targeting the MDM2 protein, known for its role in regulating p53 activity. This compound serves as a critical building block for the development of Proteolysis Targeting Chimeras (PROTACs), facilitating the selective degradation of MDM2 to enhance p53-mediated tumor suppression. MDM2 Ligand 5 is valuable for research applications focused on cancer therapeutics and the modulation of oncogenic pathways. -
MDM2-p53 Inhibitor
MDM2-p53-IN-16 is an inhibitor of the MDM2-p53 complex, demonstrating an IC50 value of 4.3 nM for the dissociation of the human p53/MDM2 interaction. By reactivating p53, it promotes apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells. This compound is suitable for use in cancer research, particularly in studies targeting p53 signaling pathways and therapeutic strategies for GBM. -
PROTAC MDM2 degrader
YX-02-030 is a PROTAC MDM2 degrader that effectively inhibits the MDM2-p53 interaction with an IC50 value of 63 nM, as well as the VHL-HIF1α binding, with an IC50 of 1.35 μM. By binding to MDM2, it recruits the VHL E3 ubiquitin ligase, promoting MDM2 degradation. This compound is particularly relevant in researching therapeutic strategies against p53 mutant or deleted triple-negative breast cancer (TNBC) cells. -
CDK2/MDM2 Inhibitor
CDK2/MDM2-IN-1 is a potent dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM for CDK2. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit key regulatory proteins positions it as a promising candidate for studies focused on cell cycle regulation and apoptosis. -
MDM2/MDMX Inhibitor
ATSP-7041 is a selective dual inhibitor of MDM2 and MDMX, designed to reactivate the p53 tumor suppressor pathway. This compound demonstrates significant biological activity in p53-positive cancers, providing a potential therapeutic strategy for tumorigenesis associated with p53 pathway dysregulation. Research applications include studying the regulation of cancer cell apoptosis and the effects of p53 reactivation on tumor growth dynamics. -
MDM2 Inhibitor
Milademetan tosylate is a potent inhibitor of MDM2, functioning through the restoration of p53 activity by disrupting the p53-MDM2 interaction. This compound effectively arrests the cell cycle in the G1 phase and induces apoptosis, demonstrating significant anticancer activity. Milademetan tosylate shows promise in research related to Merkel cell carcinoma (MCC) and other malignancies involving dysfunctional p53 signaling. -
MDM2-p53 Inhibitor
AM-7209 is a potent and selective inhibitor of the MDM2-p53 interaction, exhibiting a dissociation constant (Kd) of 38 pM. It demonstrates significant inhibitory efficacy in the MDM2-amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 is primarily utilized in cancer research for its antitumor properties, specifically in studies aimed at reactivating p53 function in malignancies where MDM2 is overexpressed. -
MDM2-p53 Inhibitor
ISA 27 is a small-molecule inhibitor of the MDM2-p53 protein-protein interaction. It effectively inhibits MDM2-mediated ubiquitination and degradation of p53, thereby stabilizing p53 levels. This compound is valuable for research on p53-mutant solid tumors, including thyroid and breast cancers, and offers a potential therapeutic strategy for targeting aberrant p53 signaling pathways. -
MDM2 Inhibitor
MDM2-IN-21 is a potent inhibitor of the MDM2 protein, which plays a critical role in the regulation of the p53 tumor suppressor pathway. By disrupting the MDM2-p53 interaction, MDM2-IN-21 activates p53-dependent signaling, leading to enhanced apoptosis and cell cycle arrest in cancer cells. This compound is widely utilized in cancer research to explore therapeutic strategies targeting MDM2 and to investigate its role in tumorigenesis and cellular responses to stress. -
MDM2/MDM4 Inhibitor
RDR03871 is a potent dual inhibitor of MDM2 and MDM4, demonstrating IC50 values of 35.4 nM and 10.4 nM for the MDM2-p53 and MDM4-p53 interactions, respectively. This compound plays a significant role in cancer research by modulating p53 pathways, thus offering a potential therapeutic avenue for tumors with dysregulated MDM2/MDM4 signaling. RDR03871 is suitable for studies focused on the restoration of p53 function in malignancies. -
MDM2-p53 Inhibitor
MI-888 TFA is a potent MDM2-p53 interaction inhibitor with a Ki of 0.44 nM, demonstrating notable efficacy in disrupting the MDM2-p53 complex. This compound exhibits rapid, complete, and sustained tumor regression in xenograft mouse models, making it a valuable tool in cancer research. MI-888 TFA is suitable for studies investigating the modulation of p53 pathways and its potential therapeutic applications in oncology. -
MDM2-p53 Inhibitor
BI-0282 is a potent inhibitor of the MDM2-p53 interaction. This compound disrupts the negative regulation of the p53 tumor suppressor by MDM2, thereby enhancing p53-mediated transcriptional activity. BI-0282 is primarily used in research applications focused on cancer therapy, specifically in studies aimed at restoring p53 function in tumor cells. Its ability to stabilize p53 makes it a valuable tool for exploring therapeutic strategies targeting MDM2 in various malignancies. -
p53-MDM2 Inhibitor
RO 2468 is a potent and selective inhibitor of the p53-MDM2 interaction, designed for oral administration. This compound exhibits significant anti-proliferative activity, effectively reducing cell growth in SJSA1 osteosarcoma models while demonstrating minimal toxicity. RO 2468 is utilized in research focused on tumor suppression and the modulation of p53 signaling pathways. -
MDM2 Inhibitor
MI-888 is a potent, orally active MDM2 inhibitor with a Ki of 0.44 nM, specifically designed to disrupt the MDM2-p53 interaction. This regulatory inhibition is critical for reactivating p53 signaling pathways, promoting apoptosis in cancer cells. With favorable pharmacokinetic properties, MI-888 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
MDM2 Inhibitor
SP-141 hydrochloride is a selective inhibitor of MDM2, a key negative regulator of the tumor suppressor p53. By promoting MDM2 auto-ubiquitination and subsequent degradation, SP-141 enhances p53 activity, which can induce apoptosis in cancer cells. This compound is primarily utilized in research focused on pancreatic and breast cancer, providing insights into MDM2-related pathways and potential therapeutic strategies. -
MDM2/4 Dual Inhibitor
YL93 is a MDM2/4 dual inhibitor, exhibiting Ki values of 0.64 μM for MDM4 and 1.1 nM for MDM2. This compound effectively induces cell-cycle arrest and promotes apoptosis in p53-dependent contexts. YL93 is valuable for research applications focused on cancer biology and the modulation of p53 signaling pathways. -
MDM2/4-p53 Inhibitor
MDM2/4-p53-IN-1 is an effective inhibitor of both MDM2-p53 and MDM4-p53 interactions, exhibiting IC50 values of 35.9 nM and 57.4 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool for cancer research and therapeutic studies targeting p53 pathways. Its ability to modulate p53 activity positions it as a promising candidate for investigations into tumorigenesis and potential cancer treatments. -
MDM2/XIAP Inhibitor
MDM2/XIAP-IN-2 is a dual inhibitor targeting murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). This compound promotes the degradation of MDM2 and interferes with XIAP mRNA translation, effectively hindering the proliferation of cancer cells. Notably, MDM2/XIAP-IN-2 demonstrates potent activity against the acute lymphoblastic leukemia cell line EU-1, with an IC50 value of 0.3 μM, making it a valuable tool for cancer research. -
MDM2 inhibitor
RG7112D is a potent MDM2 inhibitor that demonstrates IC50 values of 11 nM for MDM2-p53 and >10,000 nM for VHL-HIF1α, as assessed by HTRF assays. This compound is designed as a bi-functional molecule, YX-02-030, through an amide bond with VHL-Amine, enhancing its activity as a MDM2-PROTAC. RG7112D effectively stabilizes MDM2 protein and elevates p53 protein levels, making it a valuable tool for research in cancer biology and therapeutic applications targeting the p53 pathway. -
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. -
MDM2 Degrader
MD-265 is a potent MDM2 degrader utilizing the PROTAC (PROteolysis TArgeting Chimeras) technology. It effectively promotes the degradation of MDM2, resulting in the reactivation of the p53 tumor suppressor pathway in cancer cells with wild-type p53. Preclinical studies demonstrate that MD-265 induces complete tumor regression and enhances long-term survival in leukemia models, making it a valuable tool for cancer research and therapeutic development. -
MDM2/GSPT1 Degrader
WB156 is a dual degrader targeting MDM2 and GSPT1, facilitating their degradation through the recruitment of Cereblon (CRBN) to the ubiquitin-proteasome pathway. This compound effectively induces ubiquitination, leading to a reduction in MDM2 and GSPT1 levels, which is valuable for investigating the role of these proteins in cancer biology. WB156 holds potential for research applications in various cancer types, including leukemia. -
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. -
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. -
MDM2 Antagonist
MI-219 is an MDM2 antagonist with a Ki of 13.3 μM, specifically designed to disrupt the interaction between MDM2 and p53. This compound effectively inhibits the proliferation of FSCCL cells, demonstrated by an IC50 of 2.5 μM. MI-219 is suitable for research applications focused on cancer biology, particularly in studies exploring pathways related to tumor suppression and the p53 signaling axis. -
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. -
MDM2 Antagonist
Nutlin 1 is a potent MDM2 antagonist that reactivates the p53 pathway, playing a critical role in cell cycle regulation and apoptosis. With an IC50 of 0.26 μM, it effectively disrupts the MDM2-p53 interaction, promoting p53-mediated transcriptional activity. This compound is widely used in cancer research to explore the therapeutic potential of p53 reactivation in tumor cells. -
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.
