Nimbolide
Based on 2 publication(s) in Google Scholar
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.79%
- No. CAS: 25990-37-8
- Fòrmula: C27H30O7
- Peso molecular:466.52
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Almacenamiento:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Nimbolide
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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IF
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Histological Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
[1]|
NF-κB |
CDK4 |
CDK6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
15.56 μM
Compound: 1
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Antiproliferative activity against human A549 cell line
Antiproliferative activity against human A549 cell line
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[PMID: 16793266] |
| BC1 cell line | ED50 |
0.39 μg/mL
Compound: 1
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Cytotoxicity against human BC1 cells after 72 hrs
Cytotoxicity against human BC1 cells after 72 hrs
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[PMID: 2614419] |
| Col2 | ED50 |
0.41 μg/mL
Compound: 1
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Cytotoxicity against human Col2 cells after 72 hrs
Cytotoxicity against human Col2 cells after 72 hrs
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[PMID: 2614419] |
| HOP-62 | IC50 |
10.37 μM
Compound: 1
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Antiproliferative activity against human HOP62 cell line
Antiproliferative activity against human HOP62 cell line
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[PMID: 16793266] |
| HT-1080 | ED50 |
0.31 μg/mL
Compound: 1
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Cytotoxicity against human HT1080 cells after 48 hrs
Cytotoxicity against human HT1080 cells after 48 hrs
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[PMID: 2614419] |
| HT-29 | IC50 |
6.94 μM
Compound: 1
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Antiproliferative activity against human HT29 cell line
Antiproliferative activity against human HT29 cell line
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[PMID: 16793266] |
| KB | ED50 |
0.25 μg/mL
Compound: 1
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Cytotoxicity against human KB cells after 72 hrs
Cytotoxicity against human KB cells after 72 hrs
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[PMID: 2614419] |
| Lu1 | ED50 |
0.42 μg/mL
Compound: 1
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Cytotoxicity against human Lu1 cells
Cytotoxicity against human Lu1 cells
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[PMID: 2614419] |
| MCF7 | IC50 |
4 μM
Compound: 11o
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Antiproliferative activity against human MCF7 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 24 hrs by MTT assay
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[PMID: 33289552] |
| MDA-MB-231 | IC50 |
6 μM
Compound: 11o
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Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
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[PMID: 33289552] |
| OVCAR-5 | IC50 |
4.17 μM
Compound: 1
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Antiproliferative activity against human OVCAR5 cell line
Antiproliferative activity against human OVCAR5 cell line
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[PMID: 16793266] |
| P388 | ED50 |
0.065 μg/mL
Compound: 1
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Cytotoxicity against mouse P388 cells after 48 hrs
Cytotoxicity against mouse P388 cells after 48 hrs
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[PMID: 2614419] |
| PC-3 | IC50 |
4.59 μM
Compound: 1
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Antiproliferative activity against human PC3 cell line
Antiproliferative activity against human PC3 cell line
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[PMID: 16793266] |
| SK-MEL-2 | ED50 |
0.53 μg/mL
Compound: 1
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Cytotoxicity against human SK-MEL-2 cells after 72 hrs
Cytotoxicity against human SK-MEL-2 cells after 72 hrs
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[PMID: 2614419] |
| SW-60 | IC50 |
8.25 μM
Compound: 1
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Antiproliferative activity against human SW60 cell line
Antiproliferative activity against human SW60 cell line
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[PMID: 16793266] |
In Vitro
Nimbolide (2 μM, 1-2 h) blocks growth factor-induced phosphorylation of Akt, ERK1/2, and STAT3 in U87EGFRvIII cells[2].
Nimbolide (2-6 μM, 24 h) inhibits the IGF-I-mediated breast cancer cell proliferation in MCF-7/MDA-MB-231 cells[3].
Nimbolide (2-6 μM, 24 h) inhibits proliferation and causes G0/G1-phase arrest through repression of cyclins (A1/B/C/D1/E1) in MCF-7/MDA-MB-231 cells[3].
Nimbolide (0-6 μM, 30 min) increases the expression of DUSP4, increases E-cadherin, Snail and MMP-3 expression[4].
Nimbolide (0-6 μM, 12 h) suppresses invasion and migration of NSCLC cells[4].
Nimbolide (0-10 μM, 12 h) inhibits proliferation and induces apoptosis in colorectal cancer cells[5].
Nimbolide (10 μM, 0-12 h) inhibits NF-κB activation in HCT-116/HT-29/Caco-2 cells by a time-dependent manner[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:U87EGFRvIII cells
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Concentration:5-20 μg/μL
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Incubation Time:2-12 h
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Result:Inhibited CDK4/6 activity in a dose-dependent manner.
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Cell Line:Breast cancer cell lines (MCF-7/MDA-MB-231)
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Concentration:2-4 μM for MCF-7 cells, 4-6 μM for MDA-MB-231 cells
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Incubation Time:24 h
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Result:Decreased protein levels of IGF-IRβ, IRS-2, PI3K, β-catenin, c-Myc, N-Ras, Raf-1, Mek, pERK1/2, cyclin (A1, B, C, D1 and E1) and PCNA.
Increased p38, p21, IGFBP-3 and PTEN protein expression.
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Cell Line:Breast cancer cell lines (MCF-7/MDA-MB-231)
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Concentration:2-4 μM for MCF-7 cells, 4-6 μM for MDA-MB-231 cells
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Incubation Time:24 h
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Result:Increased the G0/G1-phase population in MCF-7 cells by 68.43 and 62.06% at 2 and 4 μM, in MDA-MB-231 cells by 57.56 and 59.35% at 4 and 6 μM.
Increased the dead cells accumulation in MCF-7 cells by 7.62 and 22.91% at 2 and 4 μM, in MDA-MB-231 cells by 6.28 and 7.73% at 4 and 6 μM.
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Cell Line:Colorectal cancer cells (HCT-116/HT-29)
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Concentration:0-10 μM
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Incubation Time:12 h
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Result:Inhibited the expression of anti-apoptotic proteins (Bcl-2/Bcl-xL/c-IAP-1/survivin) and cell proliferative proteins (cyclin D1/c-Myc).
Inhibited the expression of proteins involved in tumor cell invasion, metastasis, and angiogenesis (MMP-9, ICAM-1, CXCR4, and VEGF) in a concentration-dependent manner.
In Vivo
Nimbolide (5 mg/kg, 20 mg/kg; i.p.; daily, 10 days), inhibits tumor growth in HCT-116-derived xenograft mouse, reduces the expression of proteins involved in invasion, metastasis, and angiogenesis (MMP-9, CXCR4, ICAM-1, and VEGF)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT-116-derived xenograft mouse[5]
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Dosage:5 mg/kg, 20 mg/kg
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Administration:Intraperitoneal injection (i.p.), daily, 10 days
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Result:Suppressed tumor growth in nude mice at a dose as low as 5 mg/kg.
Reduced tumor growth by almost 90% on day 10 at a dose as low as 20 mg/kg.
Didn’t affect the body weight of mice.
Chemical Information
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No. CAS 25990-37-8
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Appearance Solid
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Peso molecular 466.52
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Fòrmula C27H30O7
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Color White to off-white
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SMILES
C[C@]12[C@@]3([H])[C@](OC([C@@]3(C=CC2=O)C)=O)([H])[C@]4([H])[C@]([C@@H]1CC(OC)=O)(C5=C(C)[C@@](C6=COC=C6)([H])C[C@@]5([H])O4)C
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Phytomedicine
A novel METTL3 inhibitor nimbolide ameliorates osteoporosis via orchestrating osteoclastogenesis in an m6A-dependent manner. [Abstract]2026 Jun:155:158048. PMID: 41865687
Nimbolide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158048. [Abstract]
CCK-8 assay in BMMs treated with increasing concentrations of Nimbolide (Nim) (0.5, 1, 3, 5, 7 μM) for 3 days and for 5 days.
Nimbolide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158048. [Abstract]
Flow cytometric analysis of apoptosis in BMMs treated with vehicle, 3 μM Nimbolide (Nim), or 5 μM Nim.
Nimbolide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158048. [Abstract]
METTL3 protein expression in RANKL-induced osteoclasts treated with low-dose Nimbolide (Nim) (5 mg/kg, i.p.) or high-dose Nim (10 mg/kg, i.p.).
Nimbolide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158048. [Abstract]
Immunofluorescence staining and quantitative analysis for m⁶A (green) and DAPI (blue) in BMMs treated with vehicle, RANKL, RANKL+Low Nimbolide (Nim) (5 mg/kg, i.p.), or RANKL+High Nim (10 mg/kg, i.p.).
Nimbolide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158048. [Abstract]
TRAP staining and quantitative analysis of TRAP-positive osteoclast number and size treated with vehicle, RANKL, RANKL+Low Nimbolide (Nim) (5 mg/kg, i.p.), or RANKL+High Nim (10 mg/kg, i.p.).
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Ecotoxicol Environ Saf
Effects of the emerging contaminant 1,3,6,8-tetrabromocarbazole on the NF-κB and correlated mechanism in human hepatocellular carcinoma cells. [Abstract]2022 Dec 1:247:114199. PMID: 36274317
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (107.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 1 mg/mL (2.14 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (289 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bodduluru LN, et al. Chemopreventive and therapeutic effects of nimbolide in cancer: the underlying mechanisms. Toxicol In Vitro. 2014 Aug;28(5):1026-35. [Content Brief]
[2]. Karkare S, et al. Direct inhibition of retinoblastoma phosphorylation by nimbolide causes cell-cycle arrest and suppresses glioblastoma growth. Clin Cancer Res. 2014 Jan 1;20(1):199-212. [Content Brief]
[3]. lumalai P, Arunkumar R, Benson CS, Sharmila G, Arunakaran J. Nimbolide inhibits IGF-I-mediated PI3K/Akt and MAPK signalling in human breast cancer cell lines (MCF-7 and MDA-MB-231). Cell Biochem Funct. 2014 Jul;32(5):476-84. [Content Brief]
[4]. Lin H, Qiu S, Xie L, Liu C, Sun S. Nimbolide suppresses non-small cell lung cancer cell invasion and migration via manipulation of DUSP4 expression and ERK1/2 signaling. Biomed Pharmacother. 2017 Aug;92:340-346. [Content Brief]
[5]. Gupta SC, Prasad S, Sethumadhavan DR, Nair MS, Mo YY, Aggarwal BB. Nimbolide, a limonoid triterpene, inhibits growth of human colorectal cancer xenografts by suppressing the proinflammatory microenvironment. Clin Cancer Res. 2013 Aug 15;19(16):4465-76. [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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1435 mL | 10.7177 mL | 21.4353 mL | 53.5883 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.2871 mL | 10.7177 mL | |
| 10 mM | 0.2144 mL | 1.0718 mL | 2.1435 mL | 5.3588 mL | |
| 15 mM | 0.1429 mL | 0.7145 mL | 1.4290 mL | 3.5726 mL | |
| 20 mM | 0.1072 mL | 0.5359 mL | 1.0718 mL | 2.6794 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8574 mL | 2.1435 mL | |
| 30 mM | 0.0715 mL | 0.3573 mL | 0.7145 mL | 1.7863 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5359 mL | 1.3397 mL | |
| 50 mM | 0.0429 mL | 0.2144 mL | 0.4287 mL | 1.0718 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3573 mL | 0.8931 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2679 mL | 0.6699 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5359 mL |
Nimbolide Related Classifications
HY-116035 Related Classifications
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