Signaling Pathway

MDM-2, p53

MDM-2, p53

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Activation of the p53 protein protects the organism against the propagation of cells that carry damaged DNA with potentially oncogenic mutations. MDM2, a p53-specific E3 ubiquitin ligase, is the principal cellular antagonist of p53, acting to limit the p53 growth-suppressive function in unstressed cells. In unstressed cells, MDM2 constantly monoubiquitinates p53 and thus is the critical step in mediating its degradation by nuclear and cytoplasmic proteasomes. The interaction between p53 and MDM2 is conformation-based and is tightly regulated on multiple levels. Disruption of the p53-MDM2 complex by multiple routes is the pivotal event for p53 activation, leading to p53 induction and its biological response. Because the p53-MDM2 interaction is structurally and biologically well understood, the design of small lipophilic molecules that disrupt or prevent it has become an important target for cancer therapy.

MDM-2, p53 Inhibitors & Modulators (29)

Product Name Catalog No. Brief Description
AMG 232

HY-12296

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).

Kevetrin hydrochloride

HY-16271

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

MI-773

HY-17493

MI-773 is an orally available spiro-oxindole HDM2 (human double minute 2) antagonist with potential antineoplastic activity.

MX69

HY-100892

MX69 is the MDM2/XIAP inhibitor, used for cancer treatment.

NSC319726

HY-18634

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

NSC59984

HY-19726

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway.

Nutlin 3

HY-50696

Nutlin-3 is MDM2 antagonist.

Nutlin 3a

HY-10029

Nutlin-3 is MDM2 antagonist.

Nutlin 3b

HY-15335

Nutlin-3b is a MDM2/p53 antagonist or inhibitor with IC50 of 13.6 μM.

NVP-CGM097

HY-15954

NVP-CGM097(CGM-097) is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity.

NVP-CGM097 stereoisomer

HY-15954A

NVP-CGM097 stereoisomer is a stereoisomer of NVP-CGM097.

p53 and MDM2 proteins-interaction-inhibitor chiral

HY-70027

p53 and MDM2 proteins-interaction-inhibitor (chiral) is an inhibitor of the interaction between p53 and MDM2 proteins.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride

HY-70027A

p53 and MDM2 proteins-interaction-inhibitor (2Hcl) is an inhibitor of the interaction between p53 and MDM2 proteins.

p53 and MDM2 proteins-interaction-inhibitor racemic

HY-70028

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

Pifithrin-α hydrobromide

HY-15484

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

Pifithrin-β

HY-16702

Pifithrin-β (Cyclic Pifithrin-α) is a potent p53 inhibitor with IC50 of 23 uM in an antiproliferative assay in the human ovarian carcinoma cell line, IGROV-1.

Pifithrin-β hydrobromide

HY-16702A

Pifithrin-β HBr (Cyclic Pifithrin-α HBr) is a potent p53 inhibitor with IC50 of 23 uM in an antiproliferative assay in the human ovarian carcinoma cell line, IGROV-1.

PRIMA-1

HY-19980A

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

Puromycin aminonucleoside

HY-15695

Puromycin Aminonucleoside (3'-Amino-3'-deoxy-N6,N6-dimethyladenosine) is the aminonucleoside portion of the antibiotic puromycin; it is a puromycin analog which does not inhibit protein synthesis or induce apoptosis.

RG7112

HY-10959

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.