RO-5963|cas 1416663-77-8|DC Chemicals

Cas No.:	1416663-77-8
Chemical Name:	(Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide
Synonyms:	RO 5963;RO5963
SMILES:	C(NC(CO)CO)(=O)C(N1C(=O)N/C(=C\C2C3=C(NC=2)C(C)=C(Cl)C=C3)/C1=O)C1=CC=C(F)C(F)=C1
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, dual MDM2/MDMX-p53 interaction inhibitor with IC50 of 17 and 24 nM, respectively; stabilizes p53 and activates the p53 pathway in cancer cells, inhibits the binding of p53 to MDM2 and MDMX; restores p53 transcriptional activity, elevates protein levels of its transcription targets, p21 and MDM2, and overcomes the apoptotic resistance of MDMX-overexpressing cell line, SJSA-X, to nutlin-3; decreases cell viability and induces cell death.

Cat. No.	Product name	Field of application
DC73117	BAY 1892005	BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit
DC70475	H203	H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively; H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.
DC8599	SP 141	SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).
DC9506	SJ-172550	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.
DC8144	Pifithrin-β (hydrobromide)	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.
DC8454	Nutlin-3a	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.
DC3125	Nutlin-3	Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
DC8746	NSC319726	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.
DC10957	MB725	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).
DC11726	Milademetan	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.