Nimbolide

SKU: orb1218260

Description

Nimbolide suppresses CDK4/CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L).

Key Properties

• CAS Number: 25990-37-8
• MW: 466.52
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₀O₇
• 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
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 50 mg/mL (107.18 mM)

Bioactivity

• In Vivo:
  Animal model: HCT-116-derived xenograft mouse. 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.
• In Vitro:
  Western blot analysis. 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. 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 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Apoptosis