MDM-2/p53 Inhibitor

p53-MDM2-IN-4 (Example 4) is an inhibitor of p53-MDM2/X protein interaction, with a K_i value of 3.079 μM. p53-MDM2-IN-4 can be used in anti-tumor research.

CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC₅₀ value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity.

Petunidin-3-O-glucoside chloride is a blood-brain barrier-penetrating tyrosinase inhibitor with an IC₅₀ of 10.3 μM and a K_i of 9.0 μM. Petunidin-3-O-glucoside also acts as an α-glucosidase inhibitor with an IC₅₀ of 218.2 µM. Petunidin-3-O-glucoside chloride inhibits the SIRT3/p53-mediated mitochondrial pathway and the PI3K/Akt-ERK pathway, suppresses glycolysis, and induces cell apoptosis. Petunidin-3-O-glucoside chloride scavenges ROS to exert antioxidant activity. It can be used in research related to glioblastoma multiforme, skin anti-aging and whitening, as well as obesity.

MMRi64 disrupts Mdm2-MdmX interactions. MMRi64 downregulates Mdm2 and MdmX in leukemia cells. MMRi64 induces p53 accumulation, and induces the apoptotic arm of the p53 pathway in leukemia/lymphoma cells. MMRi64 can be used for cancer research.

Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC₅₀ value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia).

Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC₅₀ of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.

MDM2-IN-23 (compound 5d) is an inhibitor of MDM2. MDM2-IN-23 has an IC₅₀ of 60.09 μM on MCF-7 cells.

MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with K_is of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity.

MD102 is an orally active transglutaminase 2 (TG2) inhibitor with an IC₅₀ of 0.35 μM. MD102 binds to the β-sandwich domain of TG2, disrupts the interaction between TG2 and p53, stabilizes p53, and reduces the activity of p-AKT and p-mTOR signaling pathways. MD102 induces cell apoptosis and inhibits tumor growth. MD102 can be used for the research of renal cell carcinoma.

p53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an K_i value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research.

MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC₅₀=4.4 nM; K_i=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.

Fluplatin is a prodrug composed of cisplatin and fluvastatin. Fluplatin has antitumor activity.

NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53.

Fluacrypyrim, a Miticide, is a STAT3 inhibitor. Fluacrypyrim significantly increases the protein tyrosine phosphatases(PTPs) activity. Fluacrypyrim inhibits the growth of leukemia cells by a predominant G1 arrest with significant decrease of the protein and mRNA levels of cyclin D1. Fluacrypyrim selectively inhibits STAT3 signaling, inducing growth arrest and apoptosis in STAT3-dependent cancer cells. Fluacrypyrim mitigates IR-induced hematopoietic system injury mainly by preventing apoptosis in the HSCs. Fluacrypyrim demonstrates significant analgesic and anti-inflammatory effects by inhibiting uterine smooth muscle contraction and inflammatory responses.

SF5 (2,2-Diphenylethyl isothiocyanate) is a sulforaphane analog. SF5 inhibits apoptosis by the JNK-p53-caspase pathway. SF5 can be used as a new renal protective agent for drug-resistant acute renal disease.

Cenersen (EL625) is an oligonucleotide targeting TP53. Cenersen can eliminate the activity of TP53 gain-of-function mutants and increase the sensitivity of lymphoma cells to cytotoxic chemotherapy in vitro. Cenersen can be used for the study of chronic lymphocytic leukemia (CLL).

Ischemin is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin inhibits p53-induced p21 activation with an IC₅₀ value of 5 µM. Ischemin also prevents apoptosis in ischemic cardiomyocytes. Ischemin can be used in the study of cardiovascular diseases (such as myocardial ischemia).

Seratrodast (Standard) is the analytical standard of Seratrodast. This product is intended for research and analytical applications. Seratrodast (AA 2414), an orally active antiasthmatic agent, is a thromboxane A2 receptor (TP) antagonist and ferroptosis inhibitor. Seratrodast reduces lipid ROS production, modulates the systemic xc-/GSH/GPX4 axis, and inhibits JNK phosphorylation and p53 expression. Seratrodast exhibits anti-asthmatic and anti-epileptic activity.

DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC₅₀ of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC₅₀=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice.

MK-4688 is an efficient inhibitor of the HDM2-p53 protein-protein interaction.