Catalog No.S8059 Synonyms: (-)-Nutlin-3
Molecular Weight(MW): 581.49
Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.
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Twenty-four hours after plating 1×105 Shh-EGFP cells, media was changed to serum-free media containing vehicle, 8µM Nutlin-3a, and/or Shh (3µg/mL). Cells were also transduced with lentivirus containing pLKO.1 empty vector or LentiORF-YFP-WIP1. 48 hours later, cells were fixed in 4% paraformaldehyde, permeabilized, incubated with α-WIP1 or α-Ki-67 antibody, and mounted using media containing DAPI. Scale bar, 100µm.
Oncogene, 2016, 35(42):5552-5564. Nutlin-3a purchased from Selleck.
Nutlin-3a preserved p53 expression without influencing high glucose (HG)-induced podocyte impairment. A-D: cultured podocytes were pre-treated by nutlin-3a for 2 hrs before subjected to HG treatment. Western blotting gel documents (A) and summarized data (B) showing the expression of p53 and MDM2 in podocytes under HG exposure for 24 hrs. n = 4. Western blotting gel documents (C) and summarized data (D) showing the expression of Desmin in podocytes under HG exposure for 24 hrs. n = 3. *P < 0.05 vs. Ctrl, #P < 0.05 vs. Vehl + HG. Ctrl: control; Vehl: vehicle; nutlin-3a: nutlin-3a treatment.
J Cell Mol Med, 2017. Nutlin-3a purchased from Selleck.
Protein expression of TP53 and p21 of ovarian cancer cell lines after treated with Nutlin-3a for 24, 48 and 72 hours at their corresponding IC50 as indicated. C, untreated control; *, cancer cell lines carrying TP53 mutation. Het, heterozygous TP53 mutation; hom, homozygous TP53 mutation.
PLoS One, 2015, 10(8):e0135101.. Nutlin-3a purchased from Selleck.
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Choose Selective Mdm2 Inhibitors
|Description||Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.|
|Features||Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.|
Nutlin-3a displaces p53 from the binding pocket of MDM2 and thereby releases p53 from inhibition and proteasomal degradation, leading to induction of its downstream targets, cell cycle arrest, and apoptosis. Seven days of incubation with 10 μM nutlin-3a led to >90% inhibition of NIH3T3 cells’ growth. Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) .
|In vivo||Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage . Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors. Tumors with wild-type p53 and mdm2 gene amplification will respond best to therapy with Nutlin-3a.|
Biacore studies:Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel
|In vitro||DMSO||100 mg/mL (171.97 mM)|
|Ethanol||100 mg/mL (171.97 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+55% PEG 300+ddH2O
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Frequently Asked Questions
What is the difference between S1061 (Nutlin-3) and S8059 (Nutlin-3a)?
S1061 is a racemic mixture of Nutlin3a and Nutlin3b. s8059 is the active enantiomer of Nutlin3.