MB725|CAS 2230058-99-6|p53 mutant Y220C stabilizer|DC Chemicals

Cas No.:	2230058-99-6
Chemical Name:	2-(diethylamino)-N-ethyl-5-hydroxy-6-iodo-7-(1H-pyrrol-1-yl)benzo[d]thiazole-4-carboxamide
Synonyms:	MB-725
SMILES:	S1C2=C(N3C=CC=C3)C(I)=C(O)C(C(NCC)=O)=C2N=C1N(CC)CC
Formula:	C₁₈H₂₁In₄O₂S
M.Wt:	484.356
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	References 1. Baud MGJ, et al. Eur J Med Chem. 2018 May 25;152:101-114. View Related Products by Target MDM2-p53

Description:

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); reduction of viability correlated with increased and selective transcription of p53 target genes such as BTG2, p21, PUMA, FAS, TNF, and TNFRSF10B, which promote apoptosis and cell cycle arrest, suggesting compound-mediated transcriptional activation of the Y220C mutant.

References:

References 1. Baud MGJ, et al. Eur J Med Chem. 2018 May 25;152:101-114. View Related Products by Target MDM2-p53

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.