Nutlin-3a
Based on 74 publication(s) in Google Scholar
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.13%
- CAS No.: 675576-98-4
- Formule: C30H30Cl2N4O4
- Masse moléculaire:581.49
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Nutlin-3a
More- Science. 2026 Feb 26;391(6788):eadz3121. [Abstract]
- Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
- Cancer Cell. 2023 Oct 9;41(10):1731-1748.e8. [Abstract]
- Cell. 2024 Feb 1;187(3):712-732.e38. [Abstract]
- Mol Cancer. 2024 Oct 30;23(1):242. [Abstract]
- Nat Genet. 2025 Jan;57(1):206-217. [Abstract]
- Nat Immunol. 2023 May;24(5):780-791. [Abstract]
- Nat Commun. 2024 Oct 4;15(1):8624. [Abstract]
- Nat Commun. 2022 Aug 4;13(1):4534. [Abstract]
- Cell Death Differ. 2023 Mar;30(3):779-793. [Abstract]
- Cell Death Differ. 2022 Nov;29(11):2177-2189. [Abstract]
- Adv Sci (Weinh). 2026 Jun;13(34):e16332. [Abstract]
- Adv Sci (Weinh). 2024 Jun 18:e2307751. [Abstract]
- Adv Sci (Weinh). 2024 Jun 10:e2401396. [Abstract]
- Cardiovasc Res. 2026 May 22;122(7):935-952. [Abstract]
- Nucleic Acids Res. 2025 Jun 6;53(11):gkaf465. [Abstract]
- J Adv Res. 2024 Jul 26:S2090-1232(24)00307-2. [Abstract]
- Clin Cancer Res. 2025 Jul 8. [Abstract]
- Cell Death Dis. 2025 Jun 17;16(1):452. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Jun 30;123(26):e2611131123. [Abstract]
- Proc Natl Acad Sci U S A. 2020 Jul 28;117(30):17808-17819. [Abstract]
- Cell Commun Signal. 2024 Dec 3;22(1):582. [Abstract]
- J Pharm Anal. 2025 Jan;15(1):101068. [Abstract]
- Dev Cell. 2022 Mar 14;57(5):638-653.e5. [Abstract]
- Acta Pharmacol Sin. 2025 Mar;46(3):740-750. [Abstract]
- Phytomedicine. 2026 Aug:158:158377. [Abstract]
- EMBO J. 2022 Mar 15;41(6):e108946. [Abstract]
- EMBO J. 2021 Feb 15;40(4):e104844. [Abstract]
- Free Radic Biol Med. 2025 Sep:237:503-514. [Abstract]
- Br J Pharmacol. 2022 Mar;179(5):1065-1081. [Abstract]
- Cell Rep. 2025 Nov 25;44(11):116495. [Abstract]
- Cell Rep. 2025 Aug 12;44(8):116152. [Abstract]
- Cell Rep. 2022 Aug 9;40(6):111177. [Abstract]
- Cell Rep. 2019 Apr 23;27(4):1176-1189.e5. [Abstract]
- Clin Transl Med. 2026 May;16(5):e70669. [Abstract]
- Oncogenesis. 2022 Jul 2;11(1):37. [Abstract]
- Eur J Med Chem. 2016 May 23:114:328-36. [Abstract]
- J Mater Chem B. 2017 Aug 7;5(29):5816-5834. [Abstract]
- J Ethnopharmacol. 2026 Mar 1:358:121001. [Abstract]
- Food Funct. 2025 Aug 26;16(17):6786-6799. [Abstract]
- Eur J Pharmacol. 2022 Jun 15;925:175002. [Abstract]
- Molecules. 2020 Mar 5;25(5):1162. [Abstract]
- Mol Oncol. 2022 Mar;16(5):1200-1217. [Abstract]
- Cancer Sci. 2023 Dec;114(12):4664-4676. [Abstract]
- Lab Invest. 2023 Jun;103(6):100105. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3611-3624. [Abstract]
- Oncol Res. 2024 Mar 20;32(4):753-768. [Abstract]
- J Funct Foods. 2026 Jan 31.
- Adv Ther. 2024 Jul 18.
- Oral Oncol. 2019 Nov;98:53-61. [Abstract]
- J Endocrinol. 2018 Apr;237(1):1-14. [Abstract]
- J Virol. 2023 Jun 29;97(6):e0037023. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2019 Aug;1866(8):1272-1281. [Abstract]
- Biochim Biophys Acta. 2018 Apr 26;1865(8):1034-1045. [Abstract]
- Med Oncol. 2022 Dec 16;40(1):49. [Abstract]
- Toxicol Appl Pharmacol. 2025 Sep 22:505:117578. [Abstract]
- Neurogastroenterol Motil. 2026 Apr;38(4):e70298. [Abstract]
- R Soc Open Sci. 2018 Aug 29;5(8):172376. [Abstract]
- Biochem Biophys Res Commun. 2025 May 15:770:152029. [Abstract]
- bioRxiv. 2026 Apr 1:2026.03.31.715684. [Abstract]
- bioRxiv. 2026 Mar 30.
- bioRxiv. 2026 Mar 26.
- bioRxiv. 2026 Feb 25.
- Pompeu Fabra University. 2025.
- bioRxiv. 2025 Jul 22.
- Research Square Print. 2025 May 28.
- bioRxiv. 2024 Nov 4:2024.10.08.617155. [Abstract]
- biorxiv. 2024 Jun 13.
- Research Square Preprint. 2024 Mar 28.
- Research Square Preprint. 2023 Jul 25.
- bioRxiv. 2023 Jul 27.
- Research Square Preprint. 2023 May 25.
- bioRxiv. 2020 Jun.
- University of Munich. 16. 2016 Jul.
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WB
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Cell Proliferation/Viability Assay
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RT-PCR
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WB
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WB
Activité biologique
MDM2-p53[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | GI50 |
1.6 μM
Compound: 1
|
Growth inhibition of human A2780 cells expressing MDM2 by SRB assay
Growth inhibition of human A2780 cells expressing MDM2 by SRB assay
|
[PMID: 21875801] |
| A549 | GI50 |
47.59 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
|
[PMID: 24852275] |
| A549 | IC50 |
15 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay
|
[PMID: 22940704] |
| A549 | IC50 |
15.12 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay
|
[PMID: 23046248] |
| A549 | IC50 |
1881 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human A549 cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human A549 cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| A549 | IC50 |
2049 nM
Compound: X
|
Antiproliferative activity against human A549 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human A549 cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| A549 | IC50 |
4.62 μM
Compound: Nutlin-3
|
Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 23601819] |
| A549 | IC50 |
4.62 μM
Compound: Nutlin-3
|
Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay
Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay
|
[PMID: 23611770] |
| A549 | IC50 |
7.9 μM
Compound: 7
|
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
|
[PMID: 35763424] |
| A549 | IC50 |
9.58 μM
Compound: 3
|
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
|
[PMID: 30045621] |
| HCT-116 | GI50 |
13 μM
Compound: 1
|
Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 21314128] |
| HCT-116 | GI50 |
2.1 μM
Compound: 1
|
Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay
Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay
|
[PMID: 21875801] |
| HCT-116 | GI50 |
25.6 μM
Compound: 1
|
Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay
Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay
|
[PMID: 21875801] |
| HCT-116 | GI50 |
27 μM
Compound: Nutlin-3a
|
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| HCT-116 | GI50 |
29 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
|
[PMID: 29691156] |
| HCT-116 | GI50 |
32.11 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay
|
[PMID: 24852275] |
| HCT-116 | GI50 |
34 μM
Compound: 1
|
Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 21314128] |
| HCT-116 | GI50 |
39.65 μM
Compound: Nutlin-3
|
Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay
Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay
|
[PMID: 24268795] |
| HCT-116 | GI50 |
4 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human p53 +/+ HCT116 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human p53 +/+ HCT116 cells measured after 72 hrs by MTS assay
|
10.1039/C5MD00450K |
| HCT-116 | GI50 |
47.8 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human p53 -/- HCT116 cells measured after 72 hrs by MTS assay
Antiproliferative activity against human p53 -/- HCT116 cells measured after 72 hrs by MTS assay
|
10.1039/C5MD00450K |
| HCT-116 | GI50 |
52.34 μM
Compound: Nutlin-3
|
Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay
Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay
|
[PMID: 24268795] |
| HCT-116 | GI50 |
55.7 μM
Compound: Nutlin-3a
|
Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay
|
[PMID: 24852275] |
| HCT-116 | GI50 |
8 μM
Compound: Nutlin-3a
|
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| HCT-116 | GI50 |
9 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
|
[PMID: 29691156] |
| HCT-116 | IC50 |
>20 μM
Compound: Nutlin-3a
|
Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay
Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay
|
[PMID: 30221935] |
| HCT-116 | IC50 |
1 μM
Compound: (4S,5R)-Nutlin-3
|
Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs
Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs
|
[PMID: 19856920] |
| HCT-116 | IC50 |
1 μM
Compound: 1
|
Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
|
[PMID: 25396320] |
| HCT-116 | IC50 |
1.3 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay
Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay
|
[PMID: 30221935] |
| HCT-116 | IC50 |
1.39 μM
Compound: (4S,5R)-Nutlin-3
|
Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay
Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay
|
[PMID: 19856920] |
| HCT-116 | IC50 |
1.5 μM
Compound: 1, Nutlin-3a
|
Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
|
[PMID: 24900694] |
| HCT-116 | IC50 |
1.6 μM
Compound: Nutlin-3
|
Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay
Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay
|
[PMID: 24139845] |
| HCT-116 | IC50 |
1038 nM
Compound: 7; Nutlin-3a
|
Antiproliferative activity against human HCT-116 cells harboring p53 assessed inhibition of cell growth incubated for 4 days by CCK-8 assay
Antiproliferative activity against human HCT-116 cells harboring p53 assessed inhibition of cell growth incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| HCT-116 | IC50 |
1038 nM
Compound: X
|
Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| HCT-116 | IC50 |
1366 nM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| HCT-116 | IC50 |
21.5 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 27101893] |
| HCT-116 | IC50 |
4 μM
Compound: Nutlin-3a
|
Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay
Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay
|
[PMID: 28987608] |
| HCT-116 | IC50 |
47.8 μM
Compound: Nutlin-3a
|
Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay
Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay
|
[PMID: 28987608] |
| HCT-116 | IC50 |
5 μM
Compound: 7
|
Antiproliferative activity against human HCT-116 cells
Antiproliferative activity against human HCT-116 cells
|
[PMID: 35763424] |
| HCT-116 | IC50 |
5.21 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 27101893] |
| HCT-116 | IC50 |
9.07 μM
Compound: 3
|
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
|
[PMID: 30045621] |
| HEK293 | IC50 |
>50 μM
Compound: Nutlin-3
|
Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay
Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay
|
[PMID: 25618595] |
| HEK293 | IC50 |
26.7 μM
Compound: X
|
Antiproliferative activity against HEK293 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against HEK293 cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| HeLa | IC50 |
27.5 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| HeLa | IC50 |
28.23 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human HeLa cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human HeLa cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| HeLa | IC50 |
31.43 μM
Compound: X
|
Antiproliferative activity against human HeLa cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human HeLa cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| HepG2 | GI50 |
51.31 μM
Compound: Nutlin-3
|
Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay
|
[PMID: 24268795] |
| HepG2 | IC50 |
10.2 μM
Compound: Nutlin-3
|
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
|
[PMID: 23802716] |
| HepG2 | IC50 |
2051 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human HepG2 cells harboring p53 incubated for 4 days by celltiter glo assay
Growth inhibition of human HepG2 cells harboring p53 incubated for 4 days by celltiter glo assay
|
[PMID: 38062557] |
| HepG2 | IC50 |
5.1 μM
Compound: Nutlin-3a
|
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 25479770] |
| LNCaP | IC50 |
1500 nM
Compound: 2, nutlin-3
|
Antiproliferative activity against human LnCAP cell line with wild type p53
Antiproliferative activity against human LnCAP cell line with wild type p53
|
[PMID: 16759082] |
| MCF7 | GI50 |
48.74 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 24852275] |
| MCF7 | IC50 |
11.6 μM
Compound: Nutlin-3
|
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 25618595] |
| MCF7 | IC50 |
2.9 μM
Compound: Nutlin-3
|
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
|
[PMID: 23802716] |
| MCF7 | IC50 |
3.74 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| MCF7 | IC50 |
5.01 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 27101893] |
| MCF7 | IC50 |
8.5 μM
Compound: 3
|
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
|
[PMID: 30045621] |
| MDA-MB-231 | IC50 |
23.5 μM
Compound: Nutlin-3
|
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
|
[PMID: 25618595] |
| MDA-MB-435S | IC50 |
29.6 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 27101893] |
| MOLM-13 | IC50 |
199 nM
Compound: X
|
Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay
Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay
|
[PMID: 38581730] |
| MSTO-211H | IC50 |
1028 nM
Compound: X
|
Antiproliferative activity against human MSTO-211H cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human MSTO-211H cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| MSTO-211H | IC50 |
2804 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human MSTO-211H cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human MSTO-211H cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| NCI-H1299 | IC50 |
10.4 μM
Compound: Nutlin-3a
|
Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay
Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay
|
[PMID: 30221935] |
| NCI-H1299 | IC50 |
14.7 μM
Compound: Nutlin-3
|
Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay
Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay
|
[PMID: 24139845] |
| NCI-H1299 | IC50 |
19.76 μM
Compound: 3
|
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
|
[PMID: 30045621] |
| NCI-H1299 | IC50 |
20.4 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay
Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay
|
[PMID: 22940704] |
| NCI-H1299 | IC50 |
20.48 μM
Compound: Nutlin-3a
|
Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay
Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay
|
[PMID: 23046248] |
| NCI-H460 | IC50 |
2.19 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| NCI-H460 | IC50 |
6.49 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human NCI-H460 cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human NCI-H460 cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| PA-1 | IC50 |
>60 μM
Compound: 88, Nutlin-3
|
Inhibition of Mdm2 in p53-deficient human PA-1 cells
Inhibition of Mdm2 in p53-deficient human PA-1 cells
|
10.1039/C2MD20089A |
| PA-1 | IC50 |
4.6 μM
Compound: 88, Nutlin-3
|
Inhibition of Mdm2-p53 interaction in human PA-1 cells
Inhibition of Mdm2-p53 interaction in human PA-1 cells
|
10.1039/C2MD20089A |
| PC-3 | IC50 |
20.04 μM
Compound: Nutlin-3
|
Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 23601819] |
| PC-3 | IC50 |
20.04 μM
Compound: Nutlin-3
|
Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay
Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay
|
[PMID: 23611770] |
| PC-3 | IC50 |
30.3 μM
Compound: Nutlin-3
|
Cytotoxicity against human PC3 cells after 24 hrs by MTT assay
Cytotoxicity against human PC3 cells after 24 hrs by MTT assay
|
[PMID: 23802716] |
| RKO | IC50 |
1 μM
Compound: 1
|
Cytotoxicity against human RKO cells
Cytotoxicity against human RKO cells
|
[PMID: 25396320] |
| RKO | IC50 |
1.5 μM
Compound: 1, Nutlin-3a
|
Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
|
[PMID: 24900694] |
| RKO | IC50 |
1917 nM
Compound: 7; Nutlin-3a
|
Antiproliferative activity against human RKO cells harboring p53 assessed inhibition of cell growth incubated for 4 days by CCK-8 assay
Antiproliferative activity against human RKO cells harboring p53 assessed inhibition of cell growth incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| RKO | IC50 |
2.49 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| SAOS-2 | GI50 |
18 μM
Compound: 1
|
Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 21314128] |
| SAOS-2 | IC50 |
12.1 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay
Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay
|
[PMID: 22940704] |
| SAOS-2 | IC50 |
31.62 μM
Compound: Nutlin-3a
|
Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay
Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay
|
[PMID: 23046248] |
| SAOS-2 | IC50 |
54.38 μM
Compound: Nutlin-3a
|
Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay
Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay
|
[PMID: 21996465] |
| SJSA-1 | EC50 |
22.8 μM
Compound: Nutlin 3a
|
Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay
Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay
|
[PMID: 29150077] |
| SJSA-1 | EC50 |
4.2 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay
Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay
|
[PMID: 31657556] |
| SJSA-1 | GI50 |
1.3 μM
Compound: 1
|
Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay
Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay
|
[PMID: 21875801] |
| SJSA-1 | GI50 |
2.6 μM
Compound: 1
|
Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 21314128] |
| SJSA-1 | IC50 |
0.7 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum
|
[PMID: 22524527] |
| SJSA-1 | IC50 |
1 μM
Compound: 1
|
Cytotoxicity against human SJSA1 cells
Cytotoxicity against human SJSA1 cells
|
[PMID: 25396320] |
| SJSA-1 | IC50 |
1.44 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay
Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay
|
[PMID: 30221935] |
| SJSA-1 | IC50 |
1.5 μM
Compound: 1, Nutlin-3a
|
Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
|
[PMID: 24900694] |
| SJSA-1 | IC50 |
1.9 μM
Compound: nutlin-3a
|
Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay
Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay
|
[PMID: 26985323] |
| SJSA-1 | IC50 |
1.9 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human SJSA1 cells
Antiproliferative activity against human SJSA1 cells
|
[PMID: 24656661] |
| SJSA-1 | IC50 |
7.1 μM
Compound: Nutlin-3a
|
Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
|
[PMID: 22524527] |
| SW480 | IC50 |
16.38 μM
Compound: X
|
Antiproliferative activity against human SW480 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human SW480 cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| SW480 | IC50 |
19.78 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| SW480 | IC50 |
24.08 nM
Compound: 7; Nutlin-3a
|
Growth inhibition of human SW480 cells incubated for 4 days by CCK-8 assay
Growth inhibition of human SW480 cells incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| SW-620 | GI50 |
57.04 μM
Compound: Nutlin-3
|
Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay
Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay
|
[PMID: 24268795] |
| U2OS | IC50 |
14.31 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
|
[PMID: 23046248] |
| U2OS | IC50 |
19.6 μM
Compound: Nutlin-3a
|
Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
|
[PMID: 22940704] |
| U2OS | IC50 |
24.61 μM
Compound: Nutlin-3a
|
Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
|
[PMID: 21996465] |
| U2OS | IC50 |
3.35 μM
Compound: Nutilin-3a; 9
|
Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 35420431] |
| U-937 | IC50 |
15.6 μM
Compound: Nutlin-3
|
Cytotoxicity against human U937 cells after 24 hrs by MTT assay
Cytotoxicity against human U937 cells after 24 hrs by MTT assay
|
[PMID: 23802716] |
| Vero | IC50 |
>50 μM
Compound: Nutlin-3
|
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
|
[PMID: 25618595] |
Nutlin-3a is a therapeutic which inhibits MDM2, activates wild-type p53, and induces apoptosis-as a therapeutic compound for TP53 wild-type ovarian carcinomas. Three cell lines (HOC-7, OVCA429 and A2780) with wild-type TP53 are highly sensitive to Nutlin-3a (IC50=4 to 6 μM). SKOV3 cells have an IC50 of 38 μM to Nutlin-3a. The two remaining ovarian clear cell lines (TOV21G and OVAS), both with TP53 wild-type, are relatively more sensitive to growth inhibition with Nutlin-3a (IC50=14 and 25 μm respectively) than the TP53 mutant cell lines[1]. Nutlin-3a is the active enantiomer of Nutlin-3. Nutlin-3a is a highly selective MDM2 antagonist and p53 inducer. Seven days of incubation with 10 μM Nutlin-3a leads to >90% inhibition of NIH/3T3 cells’growth but does not affect the proliferation of MEF in which both targets of the drug are eliminated. Nutlin-3a effectively arrestes cell-cycle progression in all cell lines, depleting the S-phase compartment to 0.2-2% and increasing the G1- and G2/M-phase compartments, indicating G1 and G2 arrest. The p53 targets p21 and MDM2 are elevated significantly 3 h after Nutlin-3a addition and reach maximal levels at 8 h. Nutlin-3a induces apoptosis in ≈60% of SJSA-1 and MHM cells after 40 h, which increase further after 60 h (85% and 65%, respectively)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 675576-98-4
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Appearance Solid
-
Masse moléculaire 581.49
-
Formule C30H30Cl2N4O4
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Color White to light yellow
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SMILES
O=C(N1C(C2=C(C=C(C=C2)OC)OC(C)C)=N[C@H]([C@H]1C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)Cl)N5CC(NCC5)=O
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Synonyms
Rebemadlin
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (74)
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Journal Impact Factor
-
Most Recent
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Science
Different repair pathways support intact or truncated insertions by R2 retrotransposon protein. [Abstract]2026 Feb 26;391(6788):eadz3121. PMID: 41231928 -
Cancer Cell
2024 May 13;42(5):850-868.e9. PMID: 38670091
Nutlin-3a purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
Immunoblotting of Eμ-Myc lymphoma (AF47A/560) and DHL (214DHL) cell lines pre-treated with QVD-O-Ph then S63845, venetoclax, or Nutlin-3a for indicated time points. HSP70 was used as a loading control.
Nutlin-3a purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
Cell viability assays of NTC and TP53 KO human B cell lymphoma cell lines. Cells were treated with the p53-activating drug Nutlin-3a for 24 h. Cell viability was measured by Annexin V/PI staining followed by flow cytometry. Error bars represent S.D. for three independent experiments. Student’s t-test; **=p<0.01, *=p<0.05.
Nutlin-3a purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
RTqPCR for the p53 target genes PUMA and P21 in parental DOHH2 and two independently derived Rho0 cell lines. Cells were pre-treated with the caspase inhibitor QVD-O-Ph (HY-12305), and then treated with 100 nM S63845 for 24 h or, as a comparator for potent p53 activation, treated with 10 µM of the MDM2 inhibitor Nutlin-3a (HY-10029) for 24 h. Ct values for each gene are normalized to the housekeeping gene HMBS, and fold change is shown relative to the DMSO-treated parental cell sample. Error bars represent S.E.M. for two independent experiments.
Nutlin-3a purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
Immunoblotting for p53 and PUMA in parental DOHH2 lymphoma cells and two independently derived Rho0 cell lines. Cells were pre-treated with QVD-O-Ph (HY-12305), and then treated with 100 nM S63845 or, as a control for potent p53 stabilization, treated with 10 µM Nutlin-3a (HY-10029) for 24 h. Blotting for HSP70 was used as a loading control. Representative blot shown from three independent experiments. Quantifications of p53 protein levels from three independent immunoblotting experiments are shown, relative to HSP70. Error bars represent S.D.
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Cancer Cell
Loss of p53 and mutational heterogeneity drives immune resistance in an autochthonous mouse lung cancer model with high tumor mutational burden. [Abstract]2023 Oct 9;41(10):1731-1748.e8. PMID: 37774698 -
Cell
2024 Feb 1;187(3):712-732.e38. PMID: 38194967 -
Mol Cancer
Tumour-intrinsic PDL1 signals regulate the Chk2 DNA damage response in cancer cells and mediate resistance to Chk1 inhibitors. [Abstract]2024 Oct 30;23(1):242. PMID: 39478560 -
Nat Genet
2025 Jan;57(1):206-217. PMID: 39779959 -
Nat Immunol
2023 May;24(5):780-791. PMID: 36928413 -
Nat Commun
MDM2 induces pro-inflammatory and glycolytic responses in M1 macrophages by integrating iNOS-nitric oxide and HIF-1α pathways in mice. [Abstract]2024 Oct 4;15(1):8624. PMID: 39366973 -
Nat Commun
2022 Aug 4;13(1):4534. PMID: 35927228 -
Cell Death Differ
2023 Mar;30(3):779-793. PMID: 36371602 -
Cell Death Differ
Targeting the miR-34a/LRPPRC/MDR1 axis collapse the chemoresistance in P53 inactive colorectal cancer. [Abstract]2022 Nov;29(11):2177-2189. PMID: 35484333 -
Adv Sci (Weinh)
Causal Prediction of TP53 Variant Pathogenicity Using a Perturbation-Informed Protein Language Model. [Abstract]2026 Jun;13(34):e16332. PMID: 41955512 -
Adv Sci (Weinh)
The Compromised Fanconi Anemia Pathway in Prelamin A-Expressing Cells Contributes to Replication Stress-Induced Genomic Instability. [Abstract]2024 Jun 18:e2307751. PMID: 38894550 -
Adv Sci (Weinh)
Enzalutamide Sensitizes Castration-Resistant Prostate Cancer to Copper-Mediated Cell Death. [Abstract]2024 Jun 10:e2401396. PMID: 38859590 -
Cardiovasc Res
Telomere recapping prevents pathogenic telomere-to-mitochondrial DNA communication in heart failure. [Abstract]2026 May 22;122(7):935-952. PMID: 41942104 -
Nucleic Acids Res
2025 Jun 6;53(11):gkaf465. PMID: 40479707 -
J Adv Res
Aberrant activation of p53-TRIB3 axis contributes to diabetic myocardial insulin resistance and sulforaphane protection. [Abstract]2024 Jul 26:S2090-1232(24)00307-2. PMID: 39069209 -
Clin Cancer Res
UBE2T-mediated HP1α ubiquitination enhances nucleolar function and promotes the progression of IDH1/TP53-mutant glioma. [Abstract]2025 Jul 8. PMID: 40627452 -
Cell Death Dis
Repurposing MDM2 inhibitor RG7388 for TP53-mutant NSCLC: a p53-independent pyroptotic mechanism via ROS/p-p38/NOXA/caspase-3/GSDME axis. [Abstract]2025 Jun 17;16(1):452. PMID: 40523886 -
Proc Natl Acad Sci U S A
MDM2 suppresses c-Myc synthesis by binding to the 5' mRNA translation regulatory sequence. [Abstract]2026 Jun 30;123(26):e2611131123. PMID: 42335241 -
Proc Natl Acad Sci U S A
2020 Jul 28;117(30):17808-17819. PMID: 32661168 -
Cell Commun Signal
Exercise alleviates hematopoietic stem cell injury following radiation via the carnosine/Slc15a2-p53 axis. [Abstract]2024 Dec 3;22(1):582. PMID: 39627813 -
J Pharm Anal
Ursodeoxycholic acid inhibits the uptake of cystine through SLC7A11 and impairs de novo synthesis of glutathione. [Abstract]2025 Jan;15(1):101068. PMID: 39902457 -
Dev Cell
2022 Mar 14;57(5):638-653.e5. PMID: 35245445 -
Acta Pharmacol Sin
A structure-based virtual screening identifies a novel MDM2 antagonist in the activation of the p53 signaling and inhibition of tumor growth. [Abstract]2025 Mar;46(3):740-750. PMID: 39384887 -
Phytomedicine
Yulin Yangchao formula improves premature ovarian insufficiency by inhibiting granulosa cell apoptosis through the PI3K/AKT/p53 signaling axis. [Abstract]2026 Aug:158:158377. PMID: 42284639 -
EMBO J
Pharmacological CDK4/6 inhibition reveals a p53-dependent senescent state with restricted toxicity. [Abstract]2022 Mar 15;41(6):e108946. PMID: 34985783 -
EMBO J
Centriolar distal appendages activate the centrosome-PIDDosome-p53 signalling axis via ANKRD26. [Abstract]2021 Feb 15;40(4):e104844. PMID: 33350486 -
Free Radic Biol Med
p67phox/NOX2 inhibits psoriasis by regulating the HIF-1α-glycolysis axis via p53-AMPK in keratinocytes. [Abstract]2025 Sep:237:503-514. PMID: 40516795 -
Br J Pharmacol
Established pulmonary hypertension in rats was reversed by a combination of a HIF-2α antagonist and a p53 agonist. [Abstract]2022 Mar;179(5):1065-1081. PMID: 34599843 -
Cell Rep
CDK12 inhibition reveals melanoma dependence on the RUNX1/CBFβ complex for genomic stability. [Abstract]2025 Nov 25;44(11):116495. PMID: 41176765 -
Cell Rep
53BP1 regulates p53-E2F7-dependent transcriptional gene repression and participates in the Fanconi anemia pathway. [Abstract]2025 Aug 12;44(8):116152. PMID: 40811062 -
Cell Rep
Phosphoproteomics of primary AML patient samples reveals rationale for AKT combination therapy and p53 context to overcome selinexor resistance. [Abstract]2022 Aug 9;40(6):111177. PMID: 35947955 -
Cell Rep
YAP Aggravates Inflammatory Bowel Disease by Regulating M1/M2 Macrophage Polarization and Gut Microbial Homeostasis. [Abstract]2019 Apr 23;27(4):1176-1189.e5. PMID: 31018132 -
Clin Transl Med
Oncogenic driver and therapeutic target: Prolactin signalling axis in retroperitoneal sarcoma. [Abstract]2026 May;16(5):e70669. PMID: 42083506 -
Oncogenesis
LIN28B inhibition sensitizes cells to p53-restoring PPI therapy through unleashed translational suppression. [Abstract]2022 Jul 2;11(1):37. PMID: 35780125 -
Eur J Med Chem
Design, synthesis and biological evaluation of novel benzimidazole-2-substituted phenyl or pyridine propyl ketene derivatives as antitumour agents. [Abstract]2016 May 23:114:328-36. PMID: 27017265
Nutlin-3a purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2016 May 23:114:328-36. [Abstract]
The effects of compounds A1, A7, A9 or Nutlin-3a in HCT116 cells by immunoprecipitation analysis
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J Mater Chem B
Effective co-delivery of nutlin-3a and p53 genes via core-shell microparticles for disruption of MDM2-p53 interaction and reactivation of p53 in hepatocellular carcinoma. [Abstract]2017 Aug 7;5(29):5816-5834. PMID: 32264215
Nutlin-3a purchased from MedChemExpress. Usage Cited in: J Mater Chem B. 2017 Aug 7;5(29):5816-5834. [Abstract]
Immunofluorescence staining of p53, caspase 3, and MDM2 proteins in HepG2 cells treated with microparticles loaded with nutlin-3a and β-CD-g-CS/pDNA 5 days after commencement of the treatment.
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J Ethnopharmacol
Chaihu Guizhi Ganjiang decoction attenuates chronic pancreatitis by suppressing acinar cell ferroptosis via regulating p53/SLC7A11/GPX4 pathway. [Abstract]2026 Mar 1:358:121001. PMID: 41354015 -
Food Funct
Combination of resveratrol and epirubicin to overcome chemoresistance in lung adenocarcinoma organoids: synergistic effects and translational implications. [Abstract]2025 Aug 26;16(17):6786-6799. PMID: 40755405 -
Eur J Pharmacol
Sampsonione F suppresses adipogenesis via activating p53 pathway during the mitotic clonal expansion progression of adipocyte differentiation. [Abstract]2022 Jun 15;925:175002. PMID: 35526567 -
Molecules
Design, Synthesis, and Biological Evaluation of Aromatic Amide-Substituted Benzimidazole-Derived Chalcones. The Effect of Upregulating TP53 Protein Expression. [Abstract]2020 Mar 5;25(5):1162. PMID: 32150865 -
Mol Oncol
USP22-mediated deubiquitination of PTEN inhibits pancreatic cancer progression by inducing p21 expression. [Abstract]2022 Mar;16(5):1200-1217. PMID: 34743406 -
Cancer Sci
Combination therapy with WEE1 inhibition and trifluridine/tipiracil against esophageal squamous cell carcinoma. [Abstract]2023 Dec;114(12):4664-4676. PMID: 37724648 -
Lab Invest
2023 Jun;103(6):100105. PMID: 36842278 -
J Cell Mol Med
P53/PANK1/miR-107 signalling pathway spans the gap between metabolic reprogramming and insulin resistance induced by high-fat diet. [Abstract]2020 Mar;24(6):3611-3624. PMID: 32048816 -
Oncol Res
Development of a cell adhesion-based prognostic model for multiple myeloma: Insights into chemotherapy response and potential reversal of adhesion effects. [Abstract]2024 Mar 20;32(4):753-768. PMID: 38560563 -
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Oral Oncol
Characterization of a head and neck cancer-derived cell line panel confirms the distinct TP53-proficient copy number-silent subclass. [Abstract]2019 Nov;98:53-61. PMID: 31541927 -
J Endocrinol
SRT2104 attenuates diabetes-induced aortic endothelial dysfunction via inhibition of P53. [Abstract]2018 Apr;237(1):1-14. PMID: 29371235 -
J Virol
2023 Jun 29;97(6):e0037023. PMID: 37219458 -
Biochim Biophys Acta Mol Cell Res
2019 Aug;1866(8):1272-1281. PMID: 30959066 -
Biochim Biophys Acta
2018 Apr 26;1865(8):1034-1045. PMID: 29704532 -
Med Oncol
2022 Dec 16;40(1):49. PMID: 36525117 -
Toxicol Appl Pharmacol
7,8-Dihydroxyflavone attenuates cisplatin-induced cardiomyocyte apoptosis and mitochondrial dysfunction via the p53/Nrf2 pathway. [Abstract]2025 Sep 22:505:117578. PMID: 40992637 -
Neurogastroenterol Motil
Acacetin Alleviates Loperamide-Induced Functional Constipation by Inhibiting P53-Mediated Apoptosis in Colonic Epithelial Cells. [Abstract]2026 Apr;38(4):e70298. PMID: 41913080 -
R Soc Open Sci
Loss of miR-143 and miR-145 in condyloma acuminatum promotes cellular proliferation and inhibits apoptosis by targeting NRAS. [Abstract]2018 Aug 29;5(8):172376. PMID: 30225000
Nutlin-3a purchased from MedChemExpress. Usage Cited in: R Soc Open Sci. 2018 Aug 29;5(8):172376. [Abstract]
HEKs are transfected with CRISPR/CAS9-gRNA for miR-143 or miR-145 for 48 h and then treated with nutlin-3a and Puromycin for another 24 h. The protein expression of NRAS and target genes in the PI3 K/ATK pathway is analysed by western blotting.
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Biochem Biophys Res Commun
2025 May 15:770:152029. PMID: 40382847 -
bioRxiv
Efficient Generation of Functional TCRαβ+ Cytotoxic T Cells from hiPSCs via Small-Molecule Modulation. [Abstract]2026 Apr 1:2026.03.31.715684. PMID: 41959015 -
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bioRxiv
2024 Nov 4:2024.10.08.617155. PMID: 39415993 -
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Solvant et solubilité
DMSO : ≥ 100 mg/mL (171.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 8 mg/mL (13.76 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
All 15 cell lines are plated at a density of 1×103 cells per well in 96-well plates. After 24h, media is exchanged and cells are treated with incremental concentrations of Nutlin 3a (1 μM, 5 μM, 10 μM, 25 μM, 50 μM, and 70 μM). After 72 h of incubation, WST-1 is added to each well, and a microplate reader is used at an absorbance of 450 nm to measure the number of remaining viable cells. Experiments are repeated with smaller titrations of Nutlin 3a as needed to determine the exact IC50 of cell lines. The IC50 is defined. Cell lines are again plated in a manner identical to above and treated with Nutlin 3a at their respective IC50, and WST-1 is added with cell viability measurement at 24, 48, and 72h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Nude mice bearing s.c. tumor xenografts (10 mice per group in the SJSA-1, LnCaP, and 22Rv1 study and 15 mice per group in the MHM study) are dosed orally twice daily with Nutlin 3a (50-200 mg/kg) or vehicle (1% Klucel, 0.1% Tween 80) for 2 weeks (22Rv1 and LnCap) or 3 weeks (SJSA-1 and MHM). Tumor volume is measured with a caliper and calculated. For Western blot analysis, nude mice with established SJSA-1 tumors (200-400 mm3, three animals per group are treated with three doses of Nutlin 3a at 150 mg/kg (at 0, 8, and 24 h), and tumors are harvested 3 h after the last dose. Tumor samples are flash-frozen and processed[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Crane EK, et al. Nutlin-3a: A Potential Therapeutic Opportunity for TP53 Wild-Type Ovarian Carcinomas. PLoS One. 2015 Aug 6;10(8):e0135101. [Content Brief]
[2]. Tovar C, et al. Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7197 mL | 8.5986 mL | 17.1972 mL | 42.9930 mL |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL | 8.5986 mL | |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7197 mL | 4.2993 mL | |
| 15 mM | 0.1146 mL | 0.5732 mL | 1.1465 mL | 2.8662 mL | |
| 20 mM | 0.0860 mL | 0.4299 mL | 0.8599 mL | 2.1497 mL | |
| 25 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL | |
| 30 mM | 0.0573 mL | 0.2866 mL | 0.5732 mL | 1.4331 mL | |
| 40 mM | 0.0430 mL | 0.2150 mL | 0.4299 mL | 1.0748 mL | |
| 50 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8599 mL | |
| 60 mM | 0.0287 mL | 0.1433 mL | 0.2866 mL | 0.7166 mL | |
| 80 mM | 0.0215 mL | 0.1075 mL | 0.2150 mL | 0.5374 mL | |
| 100 mM | 0.0172 mL | 0.0860 mL | 0.1720 mL | 0.4299 mL |