Catalog No.
Product Name
Application
Product Information
Citations
-
Mdm2 antagonist
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.- Maxime Parisotto, .et al. , J Exp Med, 2018, Jun 4; 215(6): 1749-1763 PMID: 29743291
- Ohmuro-Matsuyama Y, .et al. , Anal Biochem, 2018, Dec 15;563:61-66 PMID: 30316750
- Alisa A. Garaeva, .et al. , Cell Cycle, 2016, 15(1): 64-71 PMID: 26771712
- A G Evstafieva, .et al. , Cell Death Dis., 2014, 5(11): e1511. PMID: 25375376
-
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.
-
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
-
MDM2 inhibitor
MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex. - Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
-
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
-
MDM2 inhibitor
NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity. -
MDM2 degrader
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.- Lingling Chen, .et al. , Biochem Pharmacol, 2024, Nov 29:232:116688 PMID: 39617210
-
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 degrader
PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 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 degrader
PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase. -
Nutlin 3-based MDM2 ligand
Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid (MDM2 ligand 1) can be connected to the ligand for protein by a linker to form PROTACs. -
Nutlin 3-based MDM2 ligand
(4R,5S)-nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs. -
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
- Solasodine (also known as Purapuridine) is a steroidal alkaloid found in plants of the Solanaceae family. It induces apoptosis by inhibiting the p53–MDM2 complex and downregulating p21^Waf1/Cip1 and Bcl-2 proteins. Solasodine exhibits a range of biological activities, including neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic, and anti-inflammatory effects.
-
PROTAC MDM2 Degrader
MD-222 is a first-in-class PROTAC degrader targeting MDM2. This compound contains ligands for both Cereblon and MDM2, facilitating the rapid degradation of MDM2 protein and subsequent activation of wild-type p53 in cellular contexts. Due to its mechanism of action, MD-222 exhibits notable anticancer properties, making it a valuable tool for research in cancer biology and therapeutic development. -
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. -
p53 Stabilizer/MDM2 PROTAC Degrader
Seldegamadlin is a selective p53 stabilizer and an MDM2 PROTAC degrader with a DC50 of 0.4 nM. It effectively inhibits the proliferation of RS4;11 cancer cells, demonstrating an IC50 of 0.3 nM, and induces cell cycle arrest at the G2/M phase while promoting apoptosis. By upregulating p53 activity, Seldegamadlin overcomes the p53-MDM2 feedback loop, making it a valuable tool for research in hematologic and solid tumors, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). -
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. -
MDM2 Antagonist
(Rac)-Nutlin-3 is a potent antagonist of the murine double minute protein 2 (MDM2), with an IC50 of 90 nM. This compound effectively disrupts the interaction between MDM2 and p53, leading to stabilization of the p53 protein. Additionally, (Rac)-Nutlin-3 promotes cell autophagy and apoptosis, making it a valuable tool for investigating the roles of MDM2 in TP53 wild-type ovarian carcinomas and other related cancer research applications. -
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.
