2. NF-κB Autophagy
  3. IKK NF-κB Autophagy
  4. IKKβ-IN-5

IKKβ-IN-5 是一种具有口服活性和选择性的 IKKβ 抑制剂，其 IC50 值为 7.5 nM。IKKβ-IN-5 可直接抑制 IKKβ 磷酸化从而减弱 NF κB 介导的炎症与生存信号，同时促进自噬 (autophagy) 流。IKKβ-IN-5 对 IKKβ 相较于同源激酶 IKKα 展现出 6 倍的选择性。IKKβ-IN-5 通过双重机制即诱导 G₂/M 期细胞周期阻滞和激活自噬 (autophagy) 发挥强效的抗增殖作用即使在体外炎症刺激条件下亦然。IKKβ-IN-5 在体内表现出良好的药代动力学特性并抑制肿瘤生长。IKKβ-IN-5 可用于结直肠癌及其他潜在炎症驱动型恶性肿瘤的相关研究。

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IKKβ-IN-5

IKKβ-IN-5 Chemical Structure

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IKKβ-IN-5 相关抗体

Top Publications Citing Use of Products

查看 IKK 亚型特异性产品:

查看所有亚型
IKK-α IKK-β IKK IKKε TBK1

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IKKβ-IN-5 is an orally active and selective IKKβ inhibitor with an IC50 of 7.5 nM. IKKβ-IN-5 directly inhibits IKKβ phosphorylation and attenuates NF κB mediated inflammatory and survival signals while promoting autophagy flux. IKKβ-IN-5 exhibits a 6-fold selectivity forIKKβ over the homologous kinase IKKα. IKKβ-IN-5 exerts robust antiproliferative effects through a dual mechanism involving G₂/M phase cell cycle arrest and autophagy activation, even under inflammatory stimulation in vitro. IKKβ-IN-5 demonstrates favorable pharmacokinetics and suppresses tumor growth in vivo. IKKβ-IN-5 can be used for colorectal cancer and potentially other inflammation driven malignancies research[1].

IC50 & Target[1]

IKK-β

7.5 nM (IC50)

体外研究
(In Vitro)

IKKβ-IN-5 (compound LP46) (0-2 μM, 48 小时) 在 RKO 和 HCT116 细胞中表现出强效抗增殖活性且在 NCM460 细胞中具有低毒性[1]。
IKKβ-IN-5 (0.75-3.0 μM, 48 小时) 通过直接抑制 IKKβ 的磷酸化，影响 RKO 和 HCT116 细胞中 IKKβ 磷酸化及其下游靶点 IκBα 的蛋白表达[1]。
IKKβ-IN-5 (0.75-3.0 μM, 7 天) 在 RKO 和 HCT116 细胞中具有长期抗增殖效应[1]。
IKKβ-IN-5 (0.75-3.0 μM, 48 小时) 即使存在炎症刺激，仍通过双重机制 (包括诱导 G2/M 期细胞周期阻滞和激活自噬) 发挥抗增殖作用，并能够阻断 NF-κB 通路激活，从而抑制 RKO 和 HCT116 细胞中的下游炎症反应[1]。
IKKΒ-IN-5 (3 μM, 48 小时) 在 IKKβ 敲低或过表达的结直肠癌细胞中，能直接抵消 IKKβ 介导的促炎和抗自噬效应[1]。

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

IKKβ-IN-5 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT116, RKO, and NCM460 cells
Concentration: 0, 0.4 0.8, 1.2, 1.6 and 2.0 μM
Incubation Time: 48 h
Result: Exhibited potent inhibitory activity, with IC50 values of 3.94 μM for RKO and 2.59 μM for HCT116.
Showed significantly lower toxicity in NCM460 cells, with an IC50 of 21.25 μM.

Western Blot Analysis[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 48 h
Result: Significantly reduced phosphorylation of both IKKβ and IκBα in a dose-dependent manner.
Induced greater inhibition of IKKβ phosphorylation.
Had no significant impact on either the expression or phosphorylation of TAK1 or MAP3K1.

Cell Proliferation Assay[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 7 days
Result: Observed Dose-dependent suppression of colony formation.
Demonstrated superior efficacy at the highest dose.

Cell Cycle Analysis[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 48 h
Result: Revealed a significant accumulation of RKO and HCT116 cells in the G2/M phase.

Cell Proliferation Assay[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 48 h
Result: Significantly inhibited DNA synthesis in both RKO and HCT116 cells.

Western Blot Analysis[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 48 h
Result: Dose-dependently increased expression levels of key autophagy-related markers, Beclin1 and LC3A/B both markers in RKO and HCT116 cells.
Enhanced expression of Beclin1 and LC3A/ B in these cells in RKO and HCT116 cells with TNF-α (HY-P1875).
Reduced p65 expression and inhibited its nuclear translocation in a dose-dependent manner.

RT-PCR[1]

Cell Line: RKO and HCT116 cells
Concentration: 0.75, 1.5, and 3 μM
Incubation Time: 48 h
Result: Significantly down regulated the expression of TNF-α, IL-6, and IL-1β in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: IKKβ knockdown CRC cells or IKKβ overexpression CRC cells
Concentration: 3 μM
Incubation Time: 48 h
Result: Reduced the phosphorylation levels of both IκBα and p65, while concurrently increasing the expression of key autophagy markers, Beclin1 and LC3A/B and exhibited superior efficacy in inhibiting IKKβ phosphorylation and suppressing NF-κB signaling upon TNF-α stimulation in IKKβ knockdown cells.
Increased p-IκBα and p-p65 levels and reduced Beclin1 and LC3A/B expression upon TNF-α stimulation in overexpression of IKKβ cells.
Decreased NF-κB phosphorylation and restoration of autophagy-related protein levels, even under TNF-α stimulation and IKKβ-overexpressing conditions.

Cell Viability Assay[1]

Cell Line: HCT116, RKO, and NCM460 cells
Concentration: 0, 0.4 0.8, 1.2, 1.6 and 2.0 μM
Incubation Time: 48 h
Result: Exhibited potent inhibitory activity, with IC50 values of 3.94 μM for RKO and 2.59 μM for HCT116.
Showed significantly lower toxicity in NCM460 cells, with an IC50 of 21.25 μM.
分子量

417.48

Formula

C23H24FN7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

IKKβ-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

IKKβ-IN-5IKKNF-κBAutophagyIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBG?/M phase cell cycle colorectal cancerIKKβautophagyInhibitorinhibitorinhibit

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