MDM2-p53

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Cat. No.	Product Name	Field of Application
DC11637	MPK-09	A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.
DC11852	CTX-1	A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation.
DC11669	CB-002 Featured	CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.
DC11865	DS-5272	A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.
DC11834	AM-6761	A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties.
DC11836	AM-8735	A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties.
DC11830	WK-298	A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively..
DC11837	RO-5963 Featured	RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.
DC11725	BI-0252	A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.
DC11727	RO-2468	A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.
DC11728	RO-5353	A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.
DC11835	AM-8553	A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.
DC11833	TDP-665759	A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM.
DC11832	NU-8165	A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 16 uM..
DC11831	NU-8231	A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 5.3 uM in ELISA assay.
DC9793	AMG232	AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells .
DC10657	COTI-2 Featured	COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.
DC11726	Milademetan Featured	Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
DC10613	NVP-HDM201(Siremadlin ) Featured	HDM201 is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.
DC7175	JNJ-26854165 (Serdemetan) Featured	JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
DC10958	MB710	MB710 is a small-molecule p53 mutant Y220C stabilizer, binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro..
DC10957	MB725 Featured	MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM).
DC8414	MI-77301 (SAR405838) Featured	MI-77301 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
DC10074	MX69 Featured	MX69 is the MDM2/XIAP inhibitor, used for cancer treatment.
DC7879	NSC 66811	NSC 66811 is a potent MDM2 inhibitor (Ki = 120 nM).
DC8746	NSC319726 Featured	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.
DC9257	NSC59984 Featured	NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway.The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.
DC3125	Nutlin-3 Featured	Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
DC8454	Nutlin-3a Featured	Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.
DC8455	Nutlin-3b	Nutlin-3b is 150-fold less potent as an inhibitor of p53-MDM2 interaction than (−)-nutlin-3, demonstrating an IC50 value of 13.6 µM.

MDM2-p53

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