- Cat. No.
- A10657
Nutlin-3
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.
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MDM2 inhibitors disrupt the binding of mouse double minute 2 homolog (MDM2) to the tumor suppressor p53. In 1992 the MDM2 protein was shown to form a complex with p53 and inhibit p53-mediated transactivation. MDM2 is also an E3 ubiquitin ligase that promotes the rapid degradation of p53, as reported in 1997. Nutlins, reported in 2004, occupy the p53-binding pocket of MDM2 and activate the p53 pathway in cells and in vivo. Nutlin 3a is the active enantiomer of nutlin-3, and Nutlin 3b is a much weaker enantiomer used as a control. RG7112 and APG-115 are further MDM2 inhibitors, while MD-224 is a degrader that removes MDM2 protein. SJ 172550 targets the MDM2 relative MDM4 (also called MDMX).
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.
Synonyms: (-)-Nutlin-3
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.
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.
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
Synonyms: XI-006
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.
Synonyms: (+)-Nutlin-3
Nutlin 3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 uM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
Synonyms: RO5045337
RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.
APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively.
MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.
MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex.
Synonyms: thioureidobutyronitrile
Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
Synonyms: RG-7388
Idasanutlin is a potent and selective p53-MDM2 inhibitor.
AMG 232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).
Synonyms: MI 773
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 and MDM2 proteins-interaction-inhibitor chiral is an inhibitor of the interaction between p53 and MDM2 proteins.
Synonyms: p53 inhibitor (racemic)
p53 and MDM2 proteins-interaction-inhibitor racemic is an inhibitor of the interaction between p53 and MDM2 proteins.
WR 1065, a dephosphorylated metabolite of amifostine (Ethyol), can protect against the immediate and delayed effects of radiation exposure.
Synonyms: CGM097
NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
MX-69 is the MDM2/XIAP inhibitor, used for cancer treatment.
Synonyms: NVP-HDM201
HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53 with IC50s of ~17 nM and ~24 nM, respectively.
Synonyms: DS-3032
Mliademetan is a specific MDM2 inhibitor, a pharmaceutical composition for use in treating acute myeloid leukemia (AML).
Synonyms: RP 52028
PK 11195 is a 2 Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitor, and is potentially useful for the Treatment of Gliomas.
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM.