PF 184

Cat. No. 4238 3 篇引用文献 1 条评论提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective IKKβ inhibitor

化学名： 8-[[[5-Chloro-2-[3,4-dimethyl-3,4-bis(hydroxymethyl)-1-pyrrolidinyl]-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide

纯度： ≥98% (HPLC)

说明书

引用文献 (3)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PF 184

PF 184 is a potent and selective IKKβ inhibitor (IC₅₀ = 37 nM). Displays selectivity over 85 other kinases. Inhibits IL-1β-induced TNF-α production in a steroid-insensitive in vitro model of oxidative stress.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

技术数据 for PF 184

分子量	619.09
公式	C₃₂H₃₂ClFN₆O₄
储存	Store at +4°C
纯度	≥98% (HPLC)
CAS Number	1187460-81-6
PubChem ID	57519531
InChI Key	JUOWWGNRWRLBSV-MEKGRNQZSA-N
Smiles	FC(C=C4)=CC=C4N(N=C3C(N)=O)C2=C3CCC1=CC=C(NC(C5=CC(N(C6)C[C@@](C)(CO)[C@]6(CO)C)=NC=C5Cl)=O)C=C12

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PF 184

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	61.91	100

制备储备液 for PF 184

以下数据基于产品分子量 619.09。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.62 mL	8.08 mL	16.15 mL
5 mM	0.32 mL	1.62 mL	3.23 mL
10 mM	0.16 mL	0.81 mL	1.62 mL
50 mM	0.03 mL	0.16 mL	0.32 mL

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产品说明书 for PF 184

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PF 184

参考文献是支持产品生物活性的出版物。

Sommers et al (2009) Novel tight-binding inhibitory factor-κB kinase (IKK-2) inhibitors demostrate target-specific anti-inflammatory activities in cellular assays and following oral and local delivery in an in vivo model of airway inflammation. J.Pharmacol.Exp.Ther. 330 377 PMID: 19478133

If you know of a relevant reference for PF 184, please let us know.

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关键词: PF 184, PF 184 supplier, PF184, pfizer, ikk-2, NF-kappaB, NF-kB, NF-κ, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, potent, selective, inhibitors, inhibits, inhibitory, factor-kappab, αb, kinases, IkB, Kinase, NF-kB/IkB, 4238, Tocris Bioscience

3 篇 PF 184 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PF 184 的部分引用包括：

Charles et al (2020) In vitro benchmarking of NF-κB inhibitors. Eur J Pharmacol 873 172981 PMID: 32014486

Michael et al (2019) Interleukin-1β Induces mtDNA Release to Activate Innate Immune Signaling via cGAS-STING. Mol Cell 74 801-815.e6 PMID: 30952515

Mora et al (2012) Bindarit: an anti-inflammatory small molecule that modulates the NFκB pathway. Cell Cycle 11 159 PMID: 22189654

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PF 184 blocks LPS-induced TNFa production.

By Anonymous on 12/11/2018

分析类型： In Vitro

种属： Mouse

细胞系/组织： Macrophages

RAW macrophages were incubated with 1 μM PF 184 for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with PF 184.