mdm2-p53

BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.

MDM2-p53-IN-16 is a potent inhibitor of the MDM2-p53 complex, with an IC 50 value of 4.3 nM for the dissociation of the human p53/MDM2 complex. It effectively reactivates p53, leading to apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells, positioning it as a valuable agent for cancer research.

MDM2-p53-IN-20 (Compd B-11j) is a synthetic inhibitor of the MDM2-p53 interaction, which is crucial in cancer [1].

MDM2-p53-IN-1b is the MDM2-p53 interaction inhibitor.

MDM2-p53-IN-18, also known as Compd A-7b, is an inhibitor of the MDM2-p53 interaction [1].

p53-MDM2-IN-1 (Example 30), an inhibitor of the p53-MDM2/X protein interaction, exhibits a K i value of 23.35 µM and holds potential for applications in anti-tumor research.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a compound that inhibits the interaction between p53 and MDM2 proteins.

The racemic p53 and MDM2 proteins-interaction-inhibitor is an inhibitor of the interaction between p53 and MDM2 proteins.

MDM2/4-p53-IN-2 (2q) is a potent dual inhibitor of MDM2/MDM4 and activator of p53, demonstrating IC50 values of 70.7 nM for MDM2-p53 and 81.4 nM for MDM4-p53 complexes. It facilitates cell cycle regulation, promotes apoptosis, and exhibits anticancer properties [1].

MDM2/4-p53-IN-3, an inhibitor of MDM2/4-p53 protein-protein interactions (PPIs), exhibits potent activity with IC50 values of 18.5 nM for MDM2-p53 and 14.8 nM for MDM4-p53. This compound is applicable in cancer research, including studies on colon cancer [1].

p53-MDM2-IN-6, an LSM-83177 hydrazone analog, acts as an efficacious p53-MDM2 inhibitor with an IC50 of 11.08 µg/mL. This compound inhibits the p53-MDM2 interaction leading to an increase in p-53 levels while concurrently decreasing GST enzyme expression. It halts the cell cycle at the S phase and induces early and late apoptosis (Apoptosis), exhibiting antiproliferative activity against the HT29 cell line with an IC50 of 10.44 µg/mL. p53-MDM2-IN-6 holds promise for research in colorectal cancer.

p53-MDM2-IN-7 (compound 6d) (hydrochloride) is an inhibitor of the p53-MDM2 interaction, utilized in anticancer research.

p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. It exhibits antitumor activity by inhibiting the NF-κB pathway.

rel-MDM2/4-p53-IN-3 is an MDM2/4-p53 protein-protein interaction (PPI) inhibitor that acts on MDM2-p53 and MDM4-p53 with IC50 values of 18.5 nM and 14.8 nM, respectively. rel-MDM2/4-p53-IN-3 can be used to study cancers, such as colon cancer.

rel-MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/MDM4 inhibitor and p53 activator that acts on both the MDM2-p53 complex (IC50: 70.7 nM) and the MDM4-p53 complex (IC50: 81.4 nM). rel-MDM2/4-p53-IN-2 is capable of regulating cell cycle, induce apoptosis, and exhibit anti-cancer effects.

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

p53-MDM2-IN-5 (compound 5a), a robust p53-MDM2 inhibitor, effectively induces apoptosis, autophagy, and DNA damage. It also causes cell cycle arrest at the S and G2/M phases and demonstrates anti-tumor activity.

Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.

RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).

MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

DPBQ (ZINC1620467) is a p53 activator. DPBQ could activate p53 and trigger apoptosis in a polyploid-specific manner, without inhibition of topoisomerase or bind DNA.