2. NF-κB Cell Cycle/DNA Damage Apoptosis
  3. NF-κB CDK Apoptosis
  4. Nimbolide

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.

For research use only. We do not sell to patients.

Nimbolide Chemical Structure

Nimbolide Chemical Structure

CAS No. : 25990-37-8

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1 mg USD 100 In-stock
5 mg USD 280 In-stock
10 mg USD 480 In-stock
25 mg USD 1030 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Nimbolide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Nimbolide

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

NF-κB

 

CDK4

 

CDK6

 

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.

Nimbolide Related Antibodies

Western Blot Analysis[2]

Cell Line: U87EGFRvIII cells
Concentration: 5-20 μg/μL
Incubation Time: 2-12 h
Result: Inhibited CDK4/6 activity in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: Breast cancer cell lines (MCF-7/MDA-MB-231)
Concentration: 2-4 μM for MCF-7 cells, 4-6 μM for MDA-MB-231 cells
Incubation Time: 24 h
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.

Cell Viability Assay[3]

Cell Line: Breast cancer cell lines (MCF-7/MDA-MB-231)
Concentration: 2-4 μM for MCF-7 cells, 4-6 μM for MDA-MB-231 cells
Incubation Time: 24 h
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.

Western Blot Analysis[5]

Cell Line: Colorectal cancer cells (HCT-116/HT-29)
Concentration: 0-10 μM
Incubation Time: 12 h
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 (10 mg/kg, i.v., daily, 7 days) inhibits glioblastoma multiforme tumor growth in U87EGFRvⅢ xenografted mouse model[2].
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.

Animal Model: HCT-116-derived xenograft mouse[5]
Dosage: 5 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection (i.p.), daily, 10 days
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.
Molecular Weight

466.52

Formula

C27H30O7
CAS No.
Appearance

Solid

Color

White to off-white

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
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1435 mL 10.7177 mL 21.4353 mL
5 mM 0.4287 mL 2.1435 mL 4.2871 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • Protocol 1

    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.
  • Protocol 2

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

    Solubility: ≥ 1 mg/mL (2.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.72%

COA (261 KB) HNMR (140 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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
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Nimbolide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nimbolide25990-37-8NF-κBCDKApoptosisNuclear factor-κBNuclear factor-kappaBCyclin dependent kinaseCDK InhibitorU87EGFRvIII cellsERK1/2AntiproliferativeInhibitorinhibitorinhibit

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