803647-40-7

803647-40-7 structure

Name: NSC59984
Chemical Name: 1-(4-Methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-2-propen-1-one
CAS Number: 803647-40-7
Molecular Formula: C₁₂H₁₅N₃O₄
Molecular Weight: 265.265
Catalog: Signaling Pathways Apoptosis MDM-2/p53
Create Date: 2018-12-28 18:11:32
Modify Date: 2024-01-10 14:02:58
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.IC50 value: 8.38 μM (EC50, for p53-null HCT116 cells)Target: p53in vitro: NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer.in vivo: NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.

Name	1-(4-Methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-2-propen-1-one
Synonyms	(2E)-1-(4-Methyl-1-piperazinyl)-3-(5-nitro-2-furyl)-2-propen-1-one 2-Propen-1-one, 1-(4-methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-, (2E)- NSC59984

Description	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.IC50 value: 8.38 μM (EC50, for p53-null HCT116 cells)Target: p53in vitro: NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer.in vivo: NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.
Related Catalog	Signaling Pathways >> Apoptosis >> MDM-2/p53 Research Areas >> Cancer
References	[1]. Zhang S, et al. Small-Molecule NSC59984 Restores p53 Pathway Signaling and Antitumor Effects against Colorectal Cancer via p73 Activation and Degradation of Mutant p53. Cancer Res. 2015 Sep 15;75(18):3842-52.