Nutlin-3 Inhibitor CAS No. 890090-75-2

Cat. No.	Name	Size	Price
KI0119	Nutlin-3	5 mg	$176
	Nutlin-3	10 mg	$272
	Nutlin-3	25 mg	$592
	Nutlin-3	100 mg	$1552

Chemical Characteristic

Product Name	Nutlin-3
CAS No.	890090-75-2
Molecular Weight	581.5
Formula	C₃₀H₃₀Cl₂N₄O₄
Chemical Name	4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one
Smiles	N1C(=O)CN(CC1)C(=O)N1C(=NC(C1c1ccc(cc1)Cl)c1ccc(cc1)Cl)c1c(cc(cc1)OC)OC(C)C
Chemical Structure

Biological activities

Nutlin-3 is a novel small-molecule murine double minute 2 (MDM2) antagonist. Nutlin-3 induces the accumulation of p53 protein in B-cell chronic lymphocytic leukemia (B-CLL) cells as well as in primary normal cells. Nutlin-3 also induces a dose-dependent cytotoxicity on B-CLL cells and triggers the apoptotic pathway in most B-CLL samples. Nutlin-3 treatment of B-CLL cells induces a dose-dependent decrease of procaspase-3 paralleled by a progressive PARP cleavage. Nutlin-3 also induces the transcription of a cluster of p53 target genes in B-CLL cells. In addition, nutlin-3 significantly increases the mRNA steady-state levels of PCNA, CDKN1A/p21, GDF15, TP53I3/PIG3, and DDB1. ^[1] Treatment with nutlin-3 results in the rapid accumulation of TP53 protein in all wt-TP53 cell lines. Nutlin-3 inhibits cell growth and activates apoptosis in both wt-TP53 and mt-TP53 MCL cells. Nutlin-3 induces cell death in mantle cell lymphoma (MCL). Nutlin-3 results in a reduction in cell proliferation/viability, an increase in the apoptotic fraction, and cell cycle arrest in wild-type (wt) TP53 Z-138 and Granta 519 cells. ^[2] Targeted inhibition of the p53-MDM2 interaction by nutlin-3 decreases the viability of UKF-NB-3 cells in a dose- and time-dependent manner, with IC50 in the low micromolar range (at 24 hours of treatment, IC50 = 3.62 µM, 95% confidence interval (CI) = 3.04 to 4.33 µM; at 48 hours, IC50= 2.49 µM, 95% CI = 2.23 to 2.77 µM; at 72 hours, IC50= 2.03 µM, 95% CI = 1.90 to 2.16 µM). Treatment with 16 µM nutlin-3 for 24 hours results in an increase in the expression of genes in both chemosensitive UKF-NB-3 and chemoresistant UKF-NB-3^rDOX²⁰ cells. Expression of MDM2 is increased by nutlin-3 treatment to a slightly higher extent in UKF-NB-3^rDOX²⁰ cells than in UKF- NB-3 cells. Oral administration of nutlin-3 to UKF-NB-3^rDOX²⁰ xenograft-bearing mice leads to inhibition of primary tumor growth and p53 pathway activation. ^[3]

Protocols

Nutlin-3 is dissolved in absolute ethanol and stored as a 10mM stock solution in 100 µL aliquots at -20°C. ^[3]

References

[1] Secchiero P, et al. Functional integrity of the p53-mediated apoptotic pathway induced by the nongenotoxic agent nutlin-3 in B-cell chronic lymphocytic leukemia (B-CLL). Blood. 2006, 107(10): 4122-4129. [2] Tabe Y, et al. MDM2 antagonist nutlin-3 displays antiproliferative and proapoptotic activity in mantle cell lymphoma. Clin Cancer Res. 2009, 15(3): 933-942. [3] Van Maerken T, et al. Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53. J Natl Cancer Inst. 2009, 101(22): 1562-1574

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