Referencia número: HY-50696

Nutlin-3

Name: Nutlin-3
Brand: MedChemExpress
SKU: HY-50696
Price: 82.00 USD
Availability: InStock
Rating: 5 (43 reviews)

43 Cited Publications

Revisión del cliente

Based on 43 publication(s) in Google Scholar

Nutlin-3 is a commercial available p53-MDM2 inhibitor, with K_i of 90 nM.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 98.66%
No. CAS: 548472-68-0
Fòrmula: C₃₀H₃₀Cl₂N₄O₄
Peso molecular:581.49

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nutlin-3 Chemical Structure

No. CAS: 548472-68-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (43)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Nutlin-3 is a commercial available p53-MDM2 inhibitor, with K_i of 90 nM.

IC₅₀ & Target

Ki: 90 nM (p53-MDM2)^[1]

In Vitro

Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis^[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21^WAF levels and is toxic to WTp53-22RV1 cells (IC₅₀, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC₅₀, >10 μM). Nutlin-3 induces p53 and p21^WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G₁-phase fraction and decreasea S-phase fraction of all three cell lines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model^[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 548472-68-0
Appearance Solid
Peso molecular 581.49
Fòrmula C₃₀H₃₀Cl₂N₄O₄
Color White to off-white
SMILES

O=C1NCCN(C(N2[C@@H](C3=CC=C(Cl)C=C3)[C@@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (43)

All Cell Imaging/StainingBio/Physico-chemical AssayIPWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Res

Squalene Epoxidase Metabolic Dependency Is a Targetable Vulnerability in Castration-Resistant Prostate Cancer. [Abstract]

2022 Sep 2;82(17):3032-3044. PMID: 35767703

Nutlin-3 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2022 Sep 2;82(17):3032-3044. [Abstract]

Relative luciferase activities of indicated SQLE promoter reporters in C4-2 cells treated with 20 μM LY294002 or 10 μM Nutlin-3 for 12 h.
Cancer Res

A GYS2/p53 Negative Feedback Loop Restricts Tumor Growth in HBV-Related Hepatocellular Carcinoma. [Abstract]

2019 Feb 1;79(3):534-545. PMID: 30584071
Nat Commun

ReLo is a simple and rapid colocalization assay to identify and characterize direct protein-protein interactions. [Abstract]

2024 Apr 3;15(1):2875. PMID: 38570497

Nutlin-3 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Apr 3;15(1):2875. [Abstract]

Nutlin-3 (5 μM; 24 h). The interaction between p53 1–50 and MDM2 1-118 was inhibited by Nutlin-3 treatment.
Nat Commun

A fast-acting lipid checkpoint in G1 prevents mitotic defects. [Abstract]

2024 Mar 18;15(1):2441. PMID: 38499565
Cell Discov

Reprogramming of palmitic acid induced by dephosphorylation of ACOX1 promotes β-catenin palmitoylation to drive colorectal cancer progression. [Abstract]

2023 Mar 7;9(1):26. PMID: 36878899
Redox Biol

p53 and fatty acids collaborate to trigger ferroptosis via the FBXO2-FABP5 axis in colorectal cancer. [Abstract]

2026 Mar:90:104043. PMID: 41604941
Cell Death Differ

p53 transcriptionally activates DCP1B to suppress tumor progression and enhance tumor sensitivity to PI3K blockade in non-small cell lung cancer. [Abstract]

2025 Apr 9. PMID: 40200093
Cell Death Dis

DEPTOR is a direct p53 target that suppresses cell growth and chemosensitivity. [Abstract]

2020 Nov 12;11(11):976. PMID: 33184290
Cancer Lett

DAB2IP suppresses tumor malignancy by inhibiting GRP75-driven p53 ubiquitination in colon cancer. [Abstract]

2022 Apr 28:532:215588. PMID: 35150809
EBioMedicine

Zinc-finger protein p52-ZER6 accelerates colorectal cancer cell proliferation and tumour progression through promoting p53 ubiquitination. [Abstract]

2019 Oct:48:248-263. PMID: 31521611

Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct:48:248-263. [Abstract]

Nutlin-3 (5 μM; 24 h). Binding capacity of MDM2 to p53 in HCT116 cells overexpressing p52-ZER6 and treated with Nutlin-3. Cells are treated with MG132 to inhibit proteasomal degradation. Cell lysates are immunoprecipitated against anti-p53 antibody. The presence ofMDM2 is detected by immunoblotting.

Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct:48:248-263. [Abstract]

Nutlin-3 (5 μM; 24 h). p53 and p21 protein accumulation in HCT116 cells overexpressing p52-ZER6 and treated with Nutlin-3, as examined using western blotting.

Nutlin-3 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Oct:48:248-263. [Abstract]

Nutlin-3 (5 μM; 24 h). Proliferation of p52-ZER6-overexpressed HCT116 cells treated with nutlin-3, as determined by the EdU incorporation assay. Representative images were shown.
Adv Healthc Mater

Engineering Iridium Nanoclusters for Boosting Ferroptotic Cell Death by Regulating GPX4 and p53 Functions. [Abstract]

2025 Apr;14(10):e2404895. PMID: 40018815
Acta Pharmacol Sin

p52-ZER6: a determinant of tumor cell sensitivity to MDM2-p53 binding inhibitors. [Abstract]

2023 Mar;44(3):647-660. PMID: 35995868
Dev Cell

Lactate shuttling links histone lactylation to adult hippocampal neurogenesis in mice. [Abstract]

2025 Apr 21;60(8):1182-1198.e8. PMID: 39765233
Oncogene

The NPC1/USP7/p53 axis regulates cholesterol and promotes the proliferation of hepatocellular carcinoma. [Abstract]

2026 Apr;45(15):1386-1397. PMID: 41882104
Oncogene

PPM1D activity promotes cellular transformation by preventing senescence and cell death. [Abstract]

2024 Oct;43(42):3081-3093. PMID: 39237765
Int J Mol Med

Isoquercitrin protects HUVECs against high glucose‑induced apoptosis through regulating p53 proteasomal degradation. [Abstract]

2021 Jul;48(1):122. PMID: 33982778
Int J Mol Med

SIRT1 inhibits apoptosis in in vivo and in vitro models of spinal cord injury via microRNA-494. [Abstract]

2019 Apr;43(4):1758-1768. PMID: 30816451
Br J Cancer

Aberrant PJA2-CHRM3 signaling creates a therapeutic vulnerability in gastric tumor. [Abstract]

2025 Aug 26. PMID: 40858831
Cell Rep

Loss of p53 exacerbates autoimmunity by reprogramming propionyl-CoA metabolism and histone modifications in Treg cells. [Abstract]

2026 Mar 15;45(3):117084. PMID: 41838722
Cell Rep

p53-responsive CMBL reprograms glucose metabolism and suppresses cancer development by destabilizing phosphofructokinase PFKP. [Abstract]

2023 Nov 14;42(11):113426. PMID: 37967006
Anal Chem

Combining the NanaPPI Toolbox and AI-Driven Virtual Inhibitor Screening for the p53-MDM2 Interaction. [Abstract]

2025 Jul 29;97(29):15687-15697. PMID: 40624834
Int J Oncol

Targeting the TP53/MDM2 axis enhances radiation sensitivity in atypical teratoid rhabdoid tumors. [Abstract]

2022 Mar;60(3):32. PMID: 35179215
J Ethnopharmacol

Mechanism of action of Pulsatilla chinensis (Bunge) Regel compounds in hepatocellular carcinoma (HCC) treatment: An integrated analysis combining network pharmacology, molecular docking, molecular dynamics simulations and luciferase reporter gene assay. [Abstract]

2025 Aug 29:352:120176. PMID: 40543694
Eur J Pharmacol

Exendin-4 improves mitochondrial integrity against cisplatin-induced cardiac damage: Targeting p53 and NF-κB pathways. [Abstract]

2025 Nov 15:1007:178233. PMID: 41075914
Eur J Pharmacol

Hirsutine mitigates ferroptosis in podocytes of diabetic kidney disease by downregulating the p53/GPX4 signaling pathway. [Abstract]

2025 Mar 15:991:177289. PMID: 39864575
Int Immunopharmacol

Paeoniflorin mitigates iron overload-induced osteoarthritis by suppressing chondrocyte ferroptosis via the p53/SLC7A11/GPX4 pathway. [Abstract]

2025 Sep 23:162:115111. PMID: 40540898
Sci Rep

In-frame germline TP53 variant impairs p53 oligomerization and predisposes to cancer. [Abstract]

2025 Aug 19;15(1):30459. PMID: 40830167
Sci Rep

A comprehensive evaluation of pathogenic mutations in primary cutaneous melanomas, including the identification of novel loss-of-function variants. [Abstract]

2019 Nov 19;9(1):17050. PMID: 31745173
Mol Cell Biochem

APOBEC3B-driven mutations negatively regulated by P53 promote tumor progression and immunosuppressive microenvironment in prostate cancer. [Abstract]

2025 Dec 12. PMID: 41385179
Mol Oncol

PPM1D activity promotes the replication stress caused by cyclin E1 overexpression. [Abstract]

2024 Jan;18(1):6-20. PMID: 37067201
Front Mol Biosci

p53-GSDME Elevation: A Path for CDK7 Inhibition to Suppress Breast Cancer Cell Survival. [Abstract]

2021 Aug 19;8:697457. PMID: 34490348
Cell Biol Int

Isoquercetin Alleviates Diabetic Retinopathy Via Inhibiting p53-Mediated Ferroptosis. [Abstract]

2025 Jul;49(7):852-864. PMID: 40329699
Front Oncol

p53 enhances elesclomol-Cu-induced cuproptosis in hepatocellular carcinoma via FDXR-mediated FDX1 upregulation. [Abstract]

2025 Jun 24:15:1584811. PMID: 40630211
Tissue Cell

The role of HM13 expression and its relationship to PI3K/Akt and p53 signaling pathways in colorectal cancer. [Abstract]

2025 Apr:93:102702. PMID: 39755056
Mol Biol Cell

Inducible FAK loss but not FAK inhibition in endothelial cells of PYK2-null mice activates p53 tumor suppressor to prevent tumor growth. [Abstract]

2025 Jun 1;36(6):ar64. PMID: 40202821
J Cancer Res Ther

Inhibition of MDM2 by nutlin-3 decreased pyroptosis but increased apoptosis of lung carcinoma cells under 5-FU chemotherapy. [Abstract]

2025 Dec 1;21(6):1186-1197. PMID: 41452010
bioRxiv

2025 Dec 3.
Res Sq

2024 Sep 02.
bioRxiv

2024 November 06.
Res Sq

2024 Jul 12.
Research Square Print

2022 Aug.
Mater Sci Eng C Mater Biol Appl

A stimuli-responsive combination therapy for recovering p53-inactivation associated drug resistance. [Abstract]

2020 Mar:108:110403. PMID: 31923941
Oncotarget

Inhibition of WIP1 phosphatase sensitizes breast cancer cells to genotoxic stress and to MDM2 antagonist nutlin-3. [Abstract]

2016 Mar 22;7(12):14458-75. PMID: 26883108

Solvente y solubilidad

In Vitro:

Ethanol : 100 mg/mL (171.97 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (85.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7197 mL

8.5986 mL

17.1972 mL

5 mM

0.3439 mL

1.7197 mL

3.4394 mL

10 mM

0.1720 mL

0.8599 mL

1.7197 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline

Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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.

Protocol 4

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.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 15.15 mg/mL (26.05 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (292 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Yu Z, et al. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int J Mol Sci. 2014 Sep 5;15(9):15741-53. [Content Brief]

[2]. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.Cancer Biol Ther. Cancer Biol Ther. 2012 Aug;13(10):915-24. [Content Brief]

[3]. Supiot S, et al. Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. Mol Cancer Ther. 2008 Apr;7(4):993-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	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
Ethanol	100 mM	0.0172 mL	0.0860 mL	0.1720 mL	0.4299 mL

Bioz

Keywords

Nutlin-3

43 Cited Publications

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Nutlin-3

Publications Citing Use of MedChemExpress (MCE) Nutlin-3