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Catalog No.
Product Name
Application
Product Information
Citations
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MDMX Inhibitor
NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.
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MDM2 inhibitor
Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.- Sho Watanabe, .et al. , J Crohns Colitis, 2021, Feb 17 PMID: 33596306
- Shun Zhang, .et al. , BPB Reports, 2019, 2, 130-133
- Momoko Ishimine, .et al. , Dis Markers, 2018, 2018: 5280736 PMID: 29651325
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MDM2 inhibitor
MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex. -
MDM2/p53 Inhibitor
Idasanutlin is a potent and selective p53-MDM2 inhibitor. -
Mdm2 inhibitor
MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction. -
p53-MDM2 interaction inhibitor
p53 and MDM2 proteins-interaction-inhibitor chiral is an inhibitor of the interaction between p53 and MDM2 proteins. -
p53-MDM2 interaction inhibitor
p53 and MDM2 proteins-interaction-inhibitor racemic is an inhibitor of the interaction between p53 and MDM2 proteins. -
MDMX inhibitor
SJ 172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.- Saketh S Dinavahi, .et al. , Cancer Immunol Res, 2022, Jun 3;10(6):757-769 PMID: 35439317
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MDM2 inhibitor
NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity. -
MDM2 inhibitor
PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase. -
MDM2 inhibitor
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase. -
MDM2 inhibitor
Mliademetan is a specific MDM2 inhibitor, a pharmaceutical composition for use in treating acute myeloid leukemia (AML). -
HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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MDM2 Inhibitor
LQFM030 is a novel small molecule inhibitor of MDM2, primarily targeting the MDM2-p53 interaction to promote cellular apoptosis. It demonstrates concentration-dependent cytotoxicity in K562 cells with an IC50 value of 0.28 mM, inducing G0/G1 phase cell cycle arrest and enhancing Caspase activity. LQFM030 also downregulates the expression of key oncogenes and proteins, including MDM2, MDMX, p73, MYC, and NF-κB. This compound is particularly valuable in cancer research, especially in the study of leukemia. -
MDM2 Inhibitor
ASTX295 is a selective MDM2 inhibitor that effectively disrupts the MDM2-p53 interaction, exhibiting an IC50 of less than 1 nM. By activating wild-type TP53, ASTX295 induces the expression of key transcriptional targets, resulting in cell death. This compound promotes the transition of pancreatic cancer cells from senescence to apoptosis while modulating p53 and DNA damage biomarkers. ASTX295 is suitable for research applications in hematologic malignancies and pancreatic cancer. -
MDM2-MDM4 Inhibitor
MMRi62 is an MDM2-MDM4 inhibitor that promotes ferroptosis by targeting negative regulators of the tumor suppressor p53. It exhibits P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induces autophagy. MMRi62 augments reactive oxygen species levels and triggers lysosomal degradation of ferritin heavy chain (FTH1), while also facilitating the proteasomal degradation of mutant p53. Moreover, MMRi62 demonstrates efficacy in vivo by inhibiting orthotopic xenograft models of PDAC characterized by frequent KRAS and TP53 mutations, supporting its potential in cancer research applications. -
Mdm2-MdmX RING Domain Inhibitor
MMRi6 is an Mdm2-MdmX RING domain inhibitor that disrupts the RING-RING interaction between Mdm2 and MdmX. This compound effectively inhibits MdmX-stimulated Mdm2 autoubiquitination and Mdm2-MdmX-mediated polyubiquitination of p53 in vitro, while sparing NEDD4-1 autoubiquitination. MMRi6 promotes stabilization and accumulation of p53, leading to PARP cleavage in wild-type p53 Emu-myc lymphoma cells. It demonstrates growth inhibition of wild-type p53 and p53-null Emu-myc lymphoma cells with IC50 values of approximately 0.5 μM and 3 μM, respectively, making it a valuable tool for studying leukemia and lymphoma. -
MDM2 Inhibitor
Milademetan tosylate hydrate is a selective, orally active inhibitor of MDM2, primarily utilized in research focused on acute myeloid leukemia (AML) and solid tumors. This compound induces G1 cell cycle arrest, promotes cellular senescence, and triggers apoptosis, making it a valuable tool for studying the therapeutic potential in cancer treatment and the underlying mechanisms of tumor biology. -
MDM2-p53 Interaction Inhibitor
MI-1061 TFA is a potent inhibitor of the MDM2-p53 interaction, exhibiting an IC50 of 4.4 nM and a Ki of 0.16 nM. This orally bioavailable and chemically stable compound effectively activates p53, leading to apoptosis in SJSA-1 xenograft tumor tissues in murine models. MI-1061 TFA demonstrates significant anti-tumor activity, making it a valuable tool for cancer research focused on the modulation of the p53 signaling pathway. -
Mdm2-MdmX Inhibitor
MMRi64 is a selective inhibitor of the Mdm2-MdmX protein interactions. This compound downregulates Mdm2 and MdmX levels in leukemia cells, leading to increased accumulation of p53 and activation of the apoptotic pathways associated with p53. MMRi64 is a valuable tool for cancer research, particularly in the study of leukemias and lymphomas, where modulation of the p53 signaling axis is critical. -
p53-MDM2 Inhibitor
DS-5272 is an orally active inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 20 nM. This compound effectively inhibits the proliferation of SJSA-1 cells (wildtype p53, IC50 = 0.17 μM) as well as DLD-1 cells (mutant p53). DS-5272 induces cell cycle arrest and promotes apoptosis in SJSA-1 cells, while also exhibiting antitumor efficacy in vivo in mouse models. This makes DS-5272 a valuable tool for research in cancer therapeutics targeting the p53 pathway. -
MDM2-NFAT1 Inhibitor
MA242 free base is a targeted inhibitor of MDM2 and NFAT1, effectively disrupting their interaction. By binding with high affinity, MA242 promotes degradation of both proteins and suppresses NFAT1-mediated transcription of MDM2. This compound has demonstrated the ability to induce apoptosis in pancreatic cancer cell lines, providing a valuable tool for research in cancer biology and therapeutic applications, particularly in contexts where p53 is either mutated or absent. -
MDM2/4 Inhibitor
MDM2/4-p53-IN-2 is a potent dual inhibitor of MDM2 and MDM4, functioning as an activator of p53. With IC50 values of 70.7 nM and 81.4 nM for the MDM2-p53 and MDM4-p53 complexes, respectively, this compound effectively regulates the cell cycle and induces apoptosis. It demonstrates significant anticancer activity, making it a valuable tool for research focused on cancer therapeutics and the modulation of p53 signaling pathways. -
p53-MDM2 Inhibitor
p53-MDM2-IN-6 is a selective inhibitor of the p53-MDM2 interaction, demonstrating an IC50 of 11.08 µg/mL. This compound effectively induces cell cycle arrest in the S phase and promotes both early and late apoptosis in HT29 colorectal cancer cell lines, with an IC50 of 10.44 µg/mL. Its ability to elevate p53 levels while decreasing GST enzyme expression highlights its potential as a valuable tool for investigating therapeutic strategies in colorectal cancer research. -
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.
