Nimbolide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nimbolide 抑制 CDK4/CDK6 激酶活性。 Nimbolide 抑制 NF-κB、Wnt、PI3K-Akt、MAPK 和 JAK-STAT 信号通路。

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).

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 hResult: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.

Animal Model:HCT-116-derived xenograft mouseDosage: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.

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Apoptosis

Apoptosis

Apoptosis|CDK4|CDK6|NF-κB

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25990-37-8

466.52

C27H30O7

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (107.18 mM)

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(-20℃)

With Ice Pack

≥ 2 years