2. NF-κB
  3. IKK
  4. IKKβ-IN-1

IKKβ-IN-1 是一种有效且具有口服活性的 IkappaB (IKK-β) 抑制剂，IC50 为 0.20 μM。IKKβ-IN-1 可以减少小鼠巨噬细胞中 PGE2 和 TNF-α 的产生。IKKβ-IN-1 能保护小鼠免受感染性休克诱导的死亡。

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IKKβ-IN-1 Chemical Structure

IKKβ-IN-1 Chemical Structure

CAS No. : 2410423-31-1

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IKKβ-IN-1 相关抗体

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查看 IKK 亚型特异性产品:

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IKK-α IKK-β IKK IKKε TBK1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality[1].

IC50 & Target[1]

IKK-β

0.2 (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
RAW264.7 IC50
> 10 μM
Compound: 7a
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced IL-6 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced IL-6 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
[PMID: 31893550]
RAW264.7 IC50
> 10 μM
Compound: 7a
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced NO level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced NO level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay
[PMID: 31893550]
RAW264.7 IC50
> 10 μM
Compound: 7a
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs in presence of LPS by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs in presence of LPS by MTT assay
[PMID: 31893550]
RAW264.7 IC50
6.27 μM
Compound: 7a
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced TNF-alpha level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced TNF-alpha level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
[PMID: 31893550]
RAW264.7 IC50
9.83 μM
Compound: 7a
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
[PMID: 31893550]
体外研究
(In Vitro)

IKKβ-IN-1 (compound 7a) (0.1, 1 and 10 μM; 24 hours) does not show significant cytotoxicity at the tested three concentrations[1].
IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) significantly reduces PGE2 production even at the low 0.1 μM concentration, and IC50 is 9.83 μM[1].
IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) elicits 44% reduction of TNF-α production at 10 μM concentration, and IC50 is 6.27 μM[1].

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

IKKβ-IN-1 相关抗体:

Cell Viability Assay

Cell Line: RAW 264.7 macrophage cells[1]
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 hours
Result: Did not show significant cytotoxicity at the tested three concentrations.
体内研究
(In Vivo)

IKKβ-IN-1 (5 or 50 mg/kg; PO, single) exhibits an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses[1].

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

Animal Model: C57BL/6 male mice (6 or 10 weeks; LPS-induced production of the inflammatory mediators)[1]
Dosage: 5 or 50 mg/kg
Administration: PO, single (1 hour before LPS injection; survival was monitored for 36 hours)
Result: Exhibited an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses.
分子量

554.66

Formula

C31H30N4O4S
CAS 号
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-1 相关分类

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  • 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-12410423-31-1IKKIκB kinaseI kappa B kinaseIKKβPGE2TNF-αBSeptic shockInflammatoryRAW 264.7C57BL/6 miceOralInhibitorinhibitorinhibit

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